Abstract

The present application relates to the field of biochemical engineering, and discloses a composition containing eicosapentaenoic acid ethyl ester, a preparation method therefor, and a use thereof. The preparation method for the composition containing eicosapentaenoic acid ethyl ester disclosed in the present application comprises the following steps: transesterification, multi-stage molecular distillation, urea inclusion, rectification and preparative chromatographic purification. In the present application, by means of performing molecular distillation and urea inclusion before rectification, a liquid mixture can be separated, removing high-boiling-point saturated fatty acid ethyl esters and most fatty acid ethyl esters with one double bond, thereby effectively lowering the rectification temperature and preventing the formation of excessive isomers. Furthermore, the composition obtained by means of the described steps can achieve an eicosapentaenoic acid ethyl ester content of as high as 96.5 area% to 99.5 area%, with low isomer and impurity content, making it suitable for use in the preparation of food and pharmaceuticals.

IPC Classes  ?

• C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
• C07C 67/48 - SeparationPurificationStabilisationUse of additives
• C07C 67/54 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation by distillation
• C07C 67/56 - SeparationPurificationStabilisationUse of additives by solid-liquid treatmentSeparationPurificationStabilisationUse of additives by chemisorption
• C07C 69/587 - Monocarboxylic acid esters having at least two carbon-to-carbon double bonds
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61P 3/06 - Antihyperlipidemics
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A23L 33/12 - Fatty acids or derivatives thereof

Abstract

The present invention relates to a pyrrole sulfonamide antacid crystal and a preparation method therefor and the use thereof, and a pharmaceutical composition. Specifically, disclosed in the present invention is a pyrrole sulfonamide antacid crystal of a compound of formula (I), and the chemical structural formula of the crystal is as represented by formula (I), wherein n=0.1 to 2.0. The crystal form has good stability, fluidity and humidity resistance; and the preparation method for the crystal form involves a simple process, is easy to control and is suitable for large-scale production.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 35/00 - Antineoplastic agents
• A61P 31/04 - Antibacterial agents

Abstract

The present disclosure provides a purification method for 3-amino-5-methylpiperidine with amino protected by Boc. The method includes adding a solvent to the crude product of 3-amino-5-methylpiperidine with amino protected by Boc, heating until it is dissolved to obtain a mixed solution; adding an acid and an amine crystallization auxiliary to the mixed solution, stirring and dispersing to obtain a dispersed solution; cooling the dispersed solution until crystallization, separating and drying same to obtain a salt crystal of 3-amino-5-methylpiperidine with amino protected by Boc. The present disclosure improves the product characters of 3-amino-5-methylpiperidine with amino protected by Boc after salifying and crystallization, thereby improving the yield and purity of the product, at the same time, it simplifies the operation steps of salifying and crystallization of 3-amino-5-methylpiperidine with amino protected by Boc, shortens the operation time, and reduces production costs.

IPC Classes  ?

• C07D 211/56 - Nitrogen atoms

Abstract

The present disclosure provides a preparation method of carotenoid agent. The preparation method provided in present disclosure includes: mixing a suspended organic dispersion phase of a carotenoid crystal with a first organic solvent in a spiral coil of a coil heat exchanger to form a mixed solution, with the carotenoid crystal in the suspended organic phase of the carotenoid crystal being dissolved in the first organic solvent to obtain an oil phase matrix of the carotenoid dissolution solution, wherein the temperature inside the spiral coil is from 50° C. to 70° C. In the present disclosure, the carotenoid crystal is dissolved in the first organic solvent at 50° C. to 70° C., effectively avoiding the drawbacks of isomerization reaction of the carotenoid agent when it is dissolved in traditional preparation methods.

IPC Classes  ?

• C07C 45/81 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation
• C07C 7/14 - Purification, separation or stabilisation of hydrocarbonsUse of additives by crystallisationPurification or separation of the crystals
• C07C 37/84 - SeparationPurificationStabilisationUse of additives by physical treatment by crystallisation
• C07C 67/52 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation

Abstract

The present disclosure discloses a method for synthesizing quinolones intermediates by a continuous flow reaction. Specifically, according to the method, a microchannel reactor is used, which improves the selectivity and conversion rate of the reaction, and the conversion rate of compound ii is increased to more than 95% and the yield is increased to more than 85%; avoids the use of a solvent such as methanol, and methyl tert-butyl ether, etc., in the intermittent reaction process, which simplifies the post-processing method, shortens the overall operation time from about 24 hours to a few minutes, greatly improving the production efficiency, and realizing the continuity and automation of the whole process; and thus makes the product have high purity and high yield, which is suitable for industrial production.

IPC Classes  ?

• C07C 227/44 - StabilisationUse of additives
• B01J 19/00 - Chemical, physical or physico-chemical processes in generalTheir relevant apparatus
• C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups

Abstract

Provided in the present disclosure are a nemonoxacin malate active pharmaceutical ingredient with low combination impurities, and a preparation method thereof, specifically, provided in the present disclosure is a method for preparing the nemonoxacin malate active pharmaceutical ingredient, the method includes the following steps: 1) providing a C1-C3 alcohol/water mixed solvent in which nemonoxacin free base (Formula II) and D,L-malic acid are dissolved; and 2) performing cooling crystallization on a mixed solution obtained in the step 1), and then performing solid-liquid separation, washing and drying on a precipitated solid, so as to obtain the nemonoxacin malate active pharmaceutical ingredient.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings

Abstract

The present invention provides a method for preparing a chiral 4-aryl-β-amino acid derivative. The preparation method comprises hydrogenating an enamine compound having a structure as shown in Formula III in an organic solvent in the presence of a catalyst containing a transition metal and BIBOPs. The preparation method of the present invention uses a small amount of a selected asymmetric catalyst, and has a simple operation, mild reaction conditions, a high yield, a high stereoselectivity, and better industrial application and economic values.

IPC Classes  ?

• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07D 487/04 - Ortho-condensed systems
• C07C 227/32 - Preparation of optical isomers by stereospecific synthesis

Abstract

The present invention provides a high-content carotenoid compound from Adonis amurensis. The content of the total carotenoid of the carotenoid compound is higher than 95%. The content of all-trans (3S, 3′S)-carotenoid is higher than 80%. The carotenoid crystals have a high purity, and can be used in multiple forms in the fields of a dietary supplement of a human being, a food additive, a feed additive and a cosmetic product. In addition, the present invention also provides a method for manufacturing the compound.

IPC Classes  ?

• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene
• A61K 36/71 - Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
• A61Q 19/00 - Preparations for care of the skin
• A23K 20/179 - Colouring agents, e.g. pigmenting or dyeing agents
• A23L 33/105 - Plant extracts, their artificial duplicates or their derivatives
• A61K 8/9789 - Magnoliopsida [dicotyledons]

Abstract

Disclosed are a high-stability daptomycin composition for injection, and a preparation method therefor. The daptomycin composition for injection comprises daptomycin and a pharmaceutically acceptable carrier, and the pharmaceutically acceptable carrier contains a divalent metal salt, a pH regulator, and an osmotic pressure regulator; and the molar ratio of daptomycin to divalent metal salt in the daptomycin composition for injection is 1: 1.0 to 1: 3.5. The composition can be used for preparing antibacterial drugs.

IPC Classes  ?

• A61K 38/12 - Cyclic peptides
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/19 - Particulate form, e.g. powders lyophilised
• A61K 47/02 - Inorganic compounds
• A61P 31/04 - Antibacterial agents

Abstract

The present invention provides a preparation method for a carotenoid preparation having high bioavailability and high stability, comprising the following steps: a) dissolving part of a water-soluble colloid and a filling substance in water to form an aqueous phase; b) adding a carotenoid crystal to the aqueous phase and stirring for dispersion so as to form a dispersion liquid; c) loading the dispersion liquid into a first-stage grinding machine for first grinding to form a first-stage grinding liquid; d) adding the remaining water-soluble colloid and filling substance to the first-stage grinding liquid, loading same into a second grinding machine for secondary grinding to obtain a second-stage grinding liquid; and e) drying the moisture in the second-stage grinding liquid to obtain carotenoid dry powder or particles.

IPC Classes  ?

• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 31/01 - Hydrocarbons
• A61K 31/047 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
• B02C 23/36 - Adding fluid, other than for crushing or disintegrating by fluid energy the crushing or disintegrating zone being submerged in liquid

Abstract

The present invention relates to an application of pyrroloquinoline quinone (PQQ) in the preparation of a medicament used for preventing and treating acute altitude sickness and acute altitude hypoxia injury. Pyrroloquinoline quinone has the effect of preventing and treating acute high altitude hypoxia injury, and as a drug for the prevention and treatment of acute altitude sickness, the efficacy thereof is equivalent to that of acetazolamide, however acetazolamide has many toxic side effects; meanwhile, as a coenzyme, pyrroloquinoline quinone has the advantages of low toxicity and is easily acceptance by patients. In addition, by means of exhaustive swimming experiments of mice under the conditions of hypoxic exposure, PQQ has been shown to have the feature characteristics of improving the working capabilities of a subject at a high altitude, however acetazolamide has not been found to have said effect.

IPC Classes  ?

• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• C07D 471/06 - Peri-condensed systems
• A61P 39/00 - General protective or antinoxious agents

Abstract

Provided is a method for preparing a chiral 4-aryl-β-amino acid derivative. The preparation method comprises hydrogenating an enamine compound having a structure as shown in Formula III in an organic solvent in the presence of a catalyst containing a transition metal and BIBOPs. The preparation method of the present invention uses a small amount of a selected asymmetric catalyst, and has a simple operation, mild reaction conditions, a high yield, a high stereoselectivity, and better industrial application and economic values.

IPC Classes  ?

• C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07F 9/6571 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
• B01J 31/24 - Phosphines

Abstract

The present invention provides a crystal form of a thiofuran pyridazine compound, a preparation method therefor and an application thereof. The crystal form of the thiofuran pyridazine compound is (S)-2-(4-fluorophenyl)-4-(piperidine-3-aminomethyl)thieno[2,3-d]pyridazine-7-carboxamide hydrochloride of formula (I). The crystal form of the thiofuran pyridazine compound in the present invention has higher stability, is stored especially in high humidity conditions, and thus is suitable for preparing various forms of drugs.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents

Abstract

A 17β-estradiol and vitamin C molecular complex, a preparation method therefor and an application thereof. The molecular complex is formed by complexing 17β-estradiol molecules with vitamin C in a molar ratio of 0.25:1 or 0.5:1 or 0.75:1 or 1:1 or 1:0.25 or 1:0.5 or 1:0.75. Provided is a method for preparing the 17β-estradiol and vitamin C molecular complex. The 17β-estradiol and vitamin C molecular complex may be distributed to bone tissue by means of bone targeting, not only significantly improving the anti-osteoporosis activity of 17β-estradiol, but also effectively avoiding the side effects of endometrial hyperplasia and thrombosis caused when using 17β-estradiol and conjugated estrogen treatment.

IPC Classes  ?

• A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives

Abstract

A method for extracting and isolating a lutein crystal from a vegetable oil resin containing a lutein diester, comprises: dissolving lipase into deionized water to form an enzyme solution; dissolving a lutein extract into an alcohol solvent containing the deionized water to form a uniform alcohol solution; adding the enzyme solution to the alcohol solution for performing hydrolysis, and stirring same to obtain a lutein solution; filtering and performing filtration isolation on the lutein solution to obtain a crystalline; re-dissolving the crystalline into a non-polar organic solvent, and using deionized water for washing a water-soluble impurity; recycling and cooling the organic solvent to obtain a recrystallization; and isolating and drying the recrystallization to obtain the lutein crystal. In this method, selectivity is strong, reaction time is short, no waste water is produced, process is environment-friendly and suitable for industrial production, and obtained lutein crystal is high in purity and yield.

IPC Classes  ?

• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene
• C12P 23/00 - Preparation of compounds containing a cyclohexene ring having an unsaturated side chain containing at least ten carbon atoms bound by conjugated double bonds, e.g. carotenes

Abstract

The present invention discloses a method for promoting the fermentation of Gluconobacter oxydans to produce D-sorbitol dehydrogenase and pyrroloquinoline quinone. The method comprises: Gluconobacter oxydans is inoculated to a fermentation culture medium, fermented and cultured under the conditions of 28-32° C. and 150-180 rpm for 6-24 hours, the fermented solution is centrifuged, and wet bacteria are collected, thus acquiring bacteria cells containing D-sorbitol dehydrogenase and pyrroloquinoline quinone. The method promotes the synthesis of coenzyme pQQ and the enzyme activity of per unit volume D-sorbitol dehydrogenase, Gluconobacter oxydans cultured and acquired using the method is biotransformed to synthesize miglitol precursor 6-deoxy-6-amino(N-hydroxyethyl)-α-L-furan sorbose (6NSL), the conversion progress of the product 6NSL is increased by 21-35%, and a biotransformation step cycle is reduced from 48 hours to 36 hours. In addition, under a same substrate concentration (60 g/L), the cumulative concentration of the product 6NSL is increased by 10 g/L or more.

IPC Classes  ?

• C12N 1/20 - BacteriaCulture media therefor
• C12P 17/02 - Oxygen as only ring hetero atoms

Abstract

A preparation method for a carotenoid preparation having high bioavailability and high stability, comprising the following steps: a) dissolving part of a water-soluble colloid and a filling substance in water to form an aqueous phase; b) adding a carotenoid crystal to the aqueous phase and stirring for dispersion so as to form a dispersion liquid; c) loading the dispersion liquid into a first-stage abrasive for first grinding to form a first-stage grinding liquid; d) adding the remaining water-soluble colloid and filling substance to the first-stage grinding liquid, loading same into a second grinding machine for secondary grinding to obtain a second-stage grinding liquid; and e) drying the moisture in the second-stage grinding liquid to obtain carotenoid dry powder or particles.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• A23L 33/105 - Plant extracts, their artificial duplicates or their derivatives
• A23L 5/44 - Addition of dyes or pigments, e.g. in combination with optical brighteners using naturally occurring organic dyes or pigments, their artificial duplicates or their derivatives using carotenoids or xanthophylls
• A23L 2/58 - Colouring agents
• A23P 10/30 - Encapsulation of particles, e.g. foodstuff additives
• B02C 17/00 - Disintegrating by tumbling mills, i.e. mills having a container charged with the material to be disintegrated with or without special disintegrating members such as pebbles or balls

Abstract

Provided are a group of paired natural β-carotene high-yield strains, a preparation therefor, and an application thereof. The strains are Blakeslea trispora, comprising two unisexual strains, i.e., Blakeslea trispora (+) and Blakeslea trispora (-); a preservation number of a positive strain thereof is CGMCC No.16491, and a preservation number of a negative strain is CGMCC No.16492. According to the present invention, breeding is performed by means of protoplast ultraviolet mutagenesis combined with chemical mutagenesis technology, and the high-yield strains are obtained by screening a resistant mutant strain resistant to high concentration plant oil and β-ionone, and performing (+) and (-) strains pairing, primary screening, secondary screening and verification in a shake flask.

IPC Classes  ?

• C12N 1/14 - Fungi Culture media therefor
• C12P 23/00 - Preparation of compounds containing a cyclohexene ring having an unsaturated side chain containing at least ten carbon atoms bound by conjugated double bonds, e.g. carotenes
• C12R 1/645 - Fungi

Abstract

Disclosed is a separation and purification method for a vancomycin analogue (I). The method comprises: using a vancomycin crude product as a raw material, firstly using polymer matrix chromatography packing for enrichment, and then performing reverse phase silica gel matrix packing chromatography, so as to obtain a vancomycin analogue having a purity of > 80%.

IPC Classes  ?

• C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography
• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof

Abstract

Disclosed is a solid beverage containing barley leaves, comprising the following components: 15-60 wt.% of a barley leaf micro-powder, 10-50 wt.% of xylitol granules, 5-20 wt.% of a matcha powder, 1-10 wt.% of inulin, 0.5-4.0 wt.% of a konjac powder, 0.2-3.0 wt.% of silicon dioxide, and 0.1-3.0 wt.% of sucralose. The present invention also relates to a method for preparing the solid beverage, comprising the following steps: mixing a barley leaf micro-powder, inulin, a konjac powder and matcha powder, and then performing wet granulation on same to obtain granulated powders; passing the granulated powders through a 20-mesh sieve after drying same to obtain whole granules; and uniformly mixing the whole granules with xylitol granules, sucralose and silicon dioxide, and then sub-packaging same, so as to obtain the solid beverage. The solid beverage is easy and fast to dissolve, does not separate, and tastes refined and smooth.

IPC Classes  ?

• A23L 2/39 - Dry compositions

Abstract

Disclosed are a minocycline(II) p-chlorobenzene sulfonate crystal form, a preparation method therefor and the use thereof. In the current preparation process of minocycline hydrochloride, the last step, i.e. the post-treatment and purification operations of a hydrogenation reaction, is the bottleneck part of the process. The preparation method for the minocycline(II) p-chlorobenzene sulfonate crystal form of the present invention comprises the following steps: dissolving a hydrogenation azo substance in an alcohol solvent, adding an acid and a palladium carbon catalyst, displacing same with nitrogen gas, and then subjecting same to a hydrogenation reaction, then adding formaldehyde at a mass percent of 35-40%, and continuously subjecting same to a hydrogenation reaction; and after the reaction is finished, displacing same with nitrogen gas, filtering the catalyst, adding p-chlorobenzenesulfonic acid for crystallization, slowly decreasing the temperature to an endpoint temperature, and filtering and drying same. The preparation method of the present invention is simple and convenient, and stable, is suitable for industrialization, and is also beneficial for subsequent filtering and drying operations. For the prepared minocycline(II) p-chlorobenzene sulfonate crystal form, the product quality thereof is sufficient for raw material drugs for preparing minocycline hydrochloride which meets required standards.

IPC Classes  ?

• C07C 237/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups

Abstract

An application of pyrroloquinoline quinone (PQQ) in the preparation of a medicament used for preventing and treating acute altitude sickness and acute altitude hypoxia injury. Pyrroloquinoline quinone has the effect of preventing and treating acute high altitude hypoxia injury, and as a drug for the prevention and treatment of acute altitude sickness, the efficacy thereof is equivalent to that of acetazolamide, however acetazolamide has many toxic side effects; meanwhile, as a coenzyme, pyrroloquinoline quinone has the advantages of low toxicity and is easily acceptance by patients. In addition, by means of exhaustive swimming experiments of mice under the conditions of hypoxic exposure, PQQ has been shown to have the feature characteristics of improving the working capabilities of a subject at a high altitude, however acetazolamide has not been found to have said effect.

IPC Classes  ?

• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

The present invention provides a method for extracting and isolating a lutein crystal from a vegetable oil resin containing a lutein diester, comprising the following steps: a) dissolving lipase into deionized water to form an enzyme solution; b) dissolving a lutein extract into an alcohol solvent containing the deionized water to form a uniform alcohol solution; c) adding the enzyme solution to the alcohol solution for performing hydrolysis, and stirring same to obtain a lutein solution; d) filtering and performing filtration isolation on the lutein solution to obtain a crystalline; e) re-dissolving the crystalline into a non-polar organic solvent, and using the deionized water for washing a water-soluble impurity; f) recycling the organic solvent and cooling same to obtain a recrystallization; and g) isolating the recrystallization and drying same to obtain the lutein crystal. According to the present invention, the selectivity is strong, the reaction time is short, no waste water is produced, the process is environment-friendly, the obtained lutein crystal is high in purity and yield, and the method is suitable for industrial production.

IPC Classes  ?

• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene

Abstract

A spray-dried powder containing daptomycin and an industrial preparation method therefor. The industrial preparation method comprises adding water to a daptomycin bulk drug to prepare an aqueous solution of daptomycin; adding a pH regulator to form a daptomycin complex solution; and filtering the daptomycin complex solution to obtain a filtered daptomycin filtrate, then spray-drying the daptomycin filtrate to obtain a high-purity daptomycin spray-dried powder, and then directly filling the powder.

IPC Classes  ?

• A61K 38/10 - Peptides having 12 to 20 amino acids
• A61K 38/12 - Cyclic peptides
• A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides

Abstract

Disclosed are glycopeptide compounds having activity of resisting drug-resistant bacteria, conforming to glycopeptide compounds represented by general formula (I). The present invention also provides a preparation method for and an application of the glycopeptide compounds. Upon testing, compared with a second-generation glycopeptide drug oritavancin, the glycopeptide antibiotic compounds have higher inhibition activity on drug-resistant bacterial strains, especially MRSA or VRE. Further testing shows that most of the glycopeptide compounds have safety higher than that of oritavancin and can be prepared into drugs for treating or preventing diseases caused by various bacterial infections, such as skin and soft tissue infections, meningitis, sepsis, pneumonia, arthritis, peritonitis, bronchitis, and empyema.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• A61K 38/14 - Peptides containing saccharide radicalsDerivatives thereof
• A61P 31/04 - Antibacterial agents

Abstract

The present invention provides a fatty glyceride preparation method, comprising converting fatty acid short-chain alcohol ester into fatty glyceride basic mixture by sequentially carrying out a normal-pressure reaction and a vacuum reaction in the nitrogen condition in the temperature of 80° C. to 150° C.; and meanwhile adding a basic catalyst and glycerin or adding a basic catalyst and a glycerin derivative into the fatty acid short-chain alcohol ester, so as to implement a conversion from the fatty acid short-chain alcohol ester to the fatty glyceride. Conditions of the preparation method are relatively moderate, and the structure of the fatty acid is not damaged in the reactions; the yield of the glyceride is high, compositions of the glyceride are stable and controllable, glyceride products having a high content of triacylglycerol can be obtained; the process is simple, costs are low, and the fatty glyceride is applicable to industrial production.

IPC Classes  ?

• C11C 3/06 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis by esterification of fats or fatty oils with glycerol
• C07C 31/22 - Trihydroxylic alcohols, e.g. glycerol
• C07C 67/03 - Preparation of carboxylic acid esters by reacting an ester group with a hydroxy group
• C11C 3/02 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis by esterification of fatty acids with glycerol
• C07C 69/604 - Polycarboxylic acid esters, the acid moiety containing more than two carboxyl groups

Abstract

A method for promoting the fermentation of Gluconobacter oxydans to produce D-sorbitol dehydrogenase and pyrroloquinoline. The method is such that: Gluconobacter oxydans is grafted to a fermentation culture medium, fermented and cultured under the conditions of 28-32 °C and 150-180 rpm for 6-24 h, the fermented solution is centrifuged, and wet bacteria are collected, thus acquiring bacteria cells containing D-sorbitol dehydrogenase and pyrroloquinoline. The method promotes the synthesis of coenzyme pQQ and the enzyme activity of per unit volume D-sorbitol dehydogenase, Gluconobacter oxydans cultured and acquired using the method is biotransformed to synthesize miglitol precursor 6-deoxy-6-amino(N-hydroxyethyl)-α-L-furan sorbose (6NSL), the conversion progress of the product 6NSL is increased by 21-35%, and a biotransformation step cycle is reduced from 48 h to 36 h. In addition, under a same substrate concentration (60 g/L), the cumulative concentration of the product 6NSL is increased by 10 g/L or more.

IPC Classes  ?

• C12N 9/04 - Oxidoreductases (1.), e.g. luciferase acting on CHOH groups as donors, e.g. glucose oxidase, lactate dehydrogenase (1.1)
• C12N 1/20 - BacteriaCulture media therefor
• C12P 17/02 - Oxygen as only ring hetero atoms

Abstract

The present invention provides a method for drying high-stability microcapsule particles containing multiple double bonds fat soluble nutrients comprises: a) preparing a microcapsule emulsion containing multiple double bonds fat soluble nutrients, performing spray granulation on the microcapsule emulsion in a spray system (1), and meanwhile blasting air into the spray system (1), the blasted air wrapping adsorption materials, and the microcapsule emulsion being immediately solidified and sized after coming into contact with the air, so as to obtain liquid droplets having surfaces to which adsorption materials are adsorbed; b) performing fluidized drying on the liquid droplets having surfaces to which the adsorption materials are adsorbed in the step a) in a multi-stage fluidized bed system (5); c) collecting non-adsorbed adsorption materials by means of an adsorption material dust removal, recovery and circulation system; and d) collecting microcapsule particle products.

IPC Classes  ?

• B01J 13/04 - Making microcapsules or microballoons by physical processes, e.g. drying, spraying
• A23P 10/30 - Encapsulation of particles, e.g. foodstuff additives
• A61K 9/50 - Microcapsules

Abstract

A stable and liposoluble active ingredient composition, a microcapsule, and a preparation method and application thereof. The liposoluble active ingredient composition comprises tocopherol, vitamin c palmitate, and a liposoluble active ingredient, wherein a weight ratio of the tocopherol to the vitamin c palmitate is 2-8:1, and a weight ratio of a combination of the tocopherol and the vitamin c palmitate to the liposoluble active ingredient is 7-13:100.

IPC Classes  ?

• A23L 3/3544 - Organic compounds containing hetero rings
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• A61K 9/50 - Microcapsules
• A61K 8/67 - Vitamins
• A61K 8/11 - Encapsulated compositions
• A61Q 19/00 - Preparations for care of the skin

Abstract

The present invention provides a stable fat-soluble active ingredient composition, microcapsule and process for preparation and use thereof. The fat-soluble active ingredient composition comprises tocopherol, vitamin C palmitate and a fat-soluble active ingredient; wherein the weight ratio of tocopherol to vitamin C palmitate is 2-8:1, the weight ratio of a combination of tocopherol with vitamin C palmitate to the fat-soluble active ingredient is 7-13:100. The present invention obtains a novel antioxidant composition without hidden dangers for improving the stability of the fat-soluble active ingredient by screening a combination of antioxidants and adjusting their proportion and dose.

IPC Classes  ?

• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• A23K 20/174 - Vitamins
• A23L 2/52 - Adding ingredients
• A23L 33/15 - Vitamins
• A61K 31/01 - Hydrocarbons
• A61K 31/12 - Ketones
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A23L 3/3499 - Organic compounds containing oxygen with doubly-bound oxygen
• A23L 3/349 - Organic compounds containing oxygen with singly-bound oxygen
• A23P 10/30 - Encapsulation of particles, e.g. foodstuff additives
• A23L 33/155 - Vitamins A or D
• A23L 3/3544 - Organic compounds containing hetero rings
• A23K 40/30 - Shaping or working-up of animal feeding-stuffs by encapsulatingShaping or working-up of animal feeding-stuffs by coating
• A23D 7/005 - Edible oil or fat compositions containing an aqueous phase, e.g. margarines characterised by ingredients other than fatty acid triglycerides
• A23K 20/147 - Polymeric derivatives, e.g. peptides or proteins
• A23D 7/00 - Edible oil or fat compositions containing an aqueous phase, e.g. margarines
• A23K 20/163 - SugarsPolysaccharides
• A61K 8/37 - Esters of carboxylic acids
• A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
• A61K 31/07 - Retinol compounds, e.g. vitamin A
• A23D 7/02 - Edible oil or fat compositions containing an aqueous phase, e.g. margarines characterised by the production or working-up
• A23K 20/158 - Fatty acidsFatsProducts containing oils or fats
• A61K 31/201 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having one or two double bonds, e.g. oleic or linoleic acid
• A61K 8/11 - Encapsulated compositions
• A61K 8/31 - Hydrocarbons
• A61K 8/35 - Ketones, e.g. quinones, benzophenone
• A61K 8/36 - Carboxylic acidsSalts or anhydrides thereof
• A61K 8/49 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
• A61K 8/55 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing phosphorus
• A61K 8/67 - Vitamins
• A61K 9/50 - Microcapsules
• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• A61Q 19/00 - Preparations for care of the skin

Abstract

A fatty glyceride preparation method. The preparation method comprises: converting fatty acid short-chain alcohol ester into fatty glyceride basic mixture by sequentially carrying out a normal-pressure reaction and a vacuum reaction in the nitrogen condition in the temperature of 80ºC to 150ºC; and adding a basic catalyst and glycerin into the fatty acid short-chain alcohol ester or adding the basic catalyst and a glycerin derivative, so as to implement the conversion from the fatty acid short-chain alcohol ester to the fatty glyceride. Conditions of the preparation method are relatively moderate, and the structure of the fatty acid is not damaged in the reactions; the yield of the glyceride is high, compositions of the glyceride are stable and controllable, glyceride products having a high content of triacylglycerol can be obtained; the process is simple, costs are low, and the fatty glyceride is applicable to industrial production.

IPC Classes  ?

• C11C 3/06 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis by esterification of fats or fatty oils with glycerol
• C11C 3/02 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis by esterification of fatty acids with glycerol
• C07C 67/03 - Preparation of carboxylic acid esters by reacting an ester group with a hydroxy group

Abstract

A glycopeptide derivative represented by the general formula (I) and a pharmaceutically acceptable salt thereof, R1 is H, 2-alkylamine-ethyl, a substituted benzyl group, a substituted phenylpropionyl group, or a linear acyl group containing a carbon-carbon double bond; the benzene ring of the benzyl or phenylpropionyl group contains a halogen, a hydroxyl group, an amino group, a dimethylamino group, a trifluoromethyl group, or a benzene ring substituted with a halogen group, a hydroxyl group or a trifluoromethyl group; the linear acyl group contains 1-6 carbon-carbon double bonds, R2 may be OH, C1 to C5 linear amine group, wherein one end of the C1 to C5 linear amine group may have a dimethylamino group or a substituted phenyl group, and the benzene ring of the substituted phenyl group contains a halogen, a cyano group or a nitro group. The compound has good antibacterial activity, and enhanced antibacterial activity on bacteria resistant to glycopeptide antibiotics.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/14 - Peptides containing saccharide radicalsDerivatives thereof
• A61P 31/04 - Antibacterial agents
• A61K 31/70 - CarbohydratesSugarsDerivatives thereof

Abstract

Provided are a glycopeptides based derivative represented by the general formula (I) and a pharmaceutically acceptable salt thereof. R1 is H, 2-alkylamine-ethyl group, a substituted benzyl group, a substituted phenylpropionyl group or a linear acyl group containing a carbon-carbon double bond, the benzene ring of said benzyl or phenylpropionyl bearing a halogen, a hydroxyl group, an amino group, a dimethylamino group, a trifluoromethyl group, or bearing a benzene ring that is substituted by a halogen atom, a hydroxyl group, or a trifluoromethyl group; the linear acyl group containing 1 to 6 carbon-carbon double bonds; R2 is a C1 to C5 linear amine group, and the terminal of the C1 to C5 linear amine group may bear a dimethylamino group or a substituted phenyl group, the benzene ring of the substituted phenyl group bearing a halogen or a cyano group or a nitro group. The compound of the formula (I) has good antibacterial activity and an enhanced antibacterial property against the glycopeptides based antibiotic resistant bacterium.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/14 - Peptides containing saccharide radicalsDerivatives thereof
• A61P 31/04 - Antibacterial agents
• C07K 1/113 - General processes for the preparation of peptides by chemical modification of precursor peptides without change of the primary structure

Abstract

A method for preparing high-content conjugated linoleic acid (CLA) through purification of vegetable oil includes alcoholysis, purification and isomerization of vegetable oil. Alcoholysis is for preparing corresponding methyl ester or ethyl ester with glyceride; purification of methyl ester or ethyl ester is for obtaining methyl linoleate or ethyl linoleate of content over 85% through silver-based silica gel column chromatography; high-content CLA is obtained after alkali-catalyzed conjugation of methyl linoleate or ethyl linoleate, and CLA products are prepared as needed. This invention changes the status quo of preparing high-content CLA with safflower oil alone, expands sources of CLA, and develops an efficient technology for separation and purification of linoleic acid. The CLA obtained is of high purity and meets applications in pharmaceutical, health care products and other industries.

IPC Classes  ?

• C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
• C11C 3/10 - Ester interchange
• C11B 7/00 - Separation of mixtures of fats or fatty oils into their constituents, e.g. saturated oils from unsaturated oils
• C07C 67/02 - Preparation of carboxylic acid esters by interreacting ester groups, i.e. transesterification
• G01N 30/02 - Column chromatography

Abstract

The present invention relates to a preparation method for a polyunsaturated fatty acid-calcium, primarily comprising directly reacting a polyunsaturated fatty acid material with a water-soluble calcium compound to obtain a polyunsaturated fatty acid-calcium salt. The present invention has a simple technical process, short reaction time, and high reaction yield. The produced polyunsaturated fatty acid-calcium product is of high quality, and relatively less byproducts and waste water are produced. The process is overall environmentally friendly and has small safety risks, and is suitable for scaled production.

IPC Classes  ?

• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
• C11C 1/02 - Preparation of fatty acids from fats, fatty oils, or waxesRefining the fatty acids from fats or fatty oils
• C11C 3/12 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis by hydrogenation
• A23K 20/158 - Fatty acidsFatsProducts containing oils or fats

Abstract

The present invention relates to a method for preparing glyceride type polyunsaturated fatty acids. The method comprises: firstly mixing a basic catalyst with glycerol or a glyceride uniformly; then adding the mixture to a polyunsaturated fatty acid material slowly, and carrying out an esterification reaction under certain conditions to obtain glyceride type polyunsaturated fatty acids, wherein the basic catalyst is a lower aliphatic alcohol sodium/potassium or a solution thereof. The procedure of the process is simple, has mild reaction conditions, short reaction time, high yield and good quality of the obtained product.

IPC Classes  ?

• C11C 3/06 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis by esterification of fats or fatty oils with glycerol

Abstract

A method for drying high-stability microcapsule particles containing a great amount of double bond fat soluble nutrients comprises: a) preparing a microcapsule emulsion containing a great amount of double bond fat soluble nutrients, performing spray granulation on the microcapsule emulsion in a spray system (1), and meanwhile blasting air into the spray system (1), the blasted air wrapping adsorption materials, and the microcapsule emulsion being immediately solidified and sized after coming into contact with the air, so as to obtain liquid droplets having surfaces to which adsorption materials are adsorbed; b) performing fluidized drying on the liquid droplets having surfaces to which the adsorption materials are adsorbed in the step a) in a multi-stage fluidized bed system (5); c) collecting non-adsorbed adsorption materials by means of an adsorption material dust removal, recovery and circulation system; and d) collecting microcapsule particle products.

IPC Classes  ?

• B01J 13/04 - Making microcapsules or microballoons by physical processes, e.g. drying, spraying

Abstract

A method of preparing a highly stable microcapsule powder or microparticles containing a fat-soluble nutrient having increased double bonds comprises: a) dissolving the increased double bonds unsaturated fat-soluble nutrient to prepare an oil phase; b) dissolving a part of a capsule shell material into water to prepare a water phase; c) shearing the water phase and the oil phase, and mixing and emulsifying the same to obtain an emulsion; d) homogenizing, by a standard high-pressure homogenizer, the obtained emulsion to obtain an average droplet size in the emulsion at a nanometer level, thereby producing a nanometer scale emulsion; e) directly adding a remaining part of the capsule shell material into the homogenized nanometer scale emulsion, and shearing, mixing, and dissolving the same to obtain a twice-embedded emulsion; and f) performing spray granulation on the twice-embedded emulsion, and drying resultant granules to obtain the highly stable microcapsule powder or microparticles.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• A61J 3/07 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of capsules or similar small containers for oral use
• A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61K 47/42 - ProteinsPolypeptidesDegradation products thereofDerivatives thereof, e.g. albumin, gelatin or zein

Abstract

Provided is a separation and purification method for vancomycin hydrochloride of high purity. The method comprises the following steps: (1) obtaining a vancomycin hydrochloride solution from a crude vancomycin product by ion exchange chromatography and obtaining a concentrate by nanofiltration desalination and concentration; (2) adjusting the concentrate with a hydrochloric acid solution and then performing a column chromatography using a reverse chromatography column for the adjusted concentrate; (3) collecting the chromatographic solution of vancomycin to obtain a mixed chromatographic solution; (4) adjusting the mixed chromatographic solution, and separating the solution and the salts by nanofiltration desalination and concentration to obtain a concentrate; and (5) obtaining a vancomycin dry powder with a chromatographic purity of up to 99% and a pure white appearance by dehydrating and drying the concentrate of step (4), or by solvent crystallization or salting-out crystallization.

IPC Classes  ?

• C07K 1/36 - ExtractionSeparationPurification by a combination of two or more processes of different types
• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• A61K 38/14 - Peptides containing saccharide radicalsDerivatives thereof
• C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography
• C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis

Abstract

The present invention provides a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, low toxicity, high anticancer activity and good stability.

IPC Classes  ?

• A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
• A61K 31/52 - Purines, e.g. adenine
• C07D 473/00 - Heterocyclic compounds containing purine ring systems
• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 473/16 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms

Abstract

Provided is a butterfly valve, said butterfly valve comprising a valve body (1) and a valve plate (2) located inside the valve body (1); the valve body (1) is equipped with at least one sprayer (3) used for purging the inside surface of the butterfly valve, and the sprayer (3) is connected to an inlet valve (4) located outside the butterfly valve; the middle of the valve plate (2) is provided with a water drainage reservoir (111) disposed in the horizontal direction; one end of the water drainage reservoir (111) is closed, and the other end is open, forming a water outlet end; the valve plate (2) is provided with at least one water drainage hole (112) in communication with the water drainage reservoir (111); the sprayer (3) is located above the water drainage reservoir (111). The sterile powder delivery apparatus consisting of a plurality of butterfly valves, and method for use thereof, feed into a corresponding medium after delivery of the powder is complete, and clean, sterilize, and dry the non-sterile areas of the butterfly valve assembly, such that sterile docking can be achieved multiple times.

IPC Classes  ?

• B65G 53/46 - Gates or sluices, e.g. rotary wheels

Abstract

The present invention relates to a method for preparing glyceride type polyunsaturated fatty acids. The preparation method comprises: firstly mixing a basic catalyst with glycerol or a glyceride uniformly; then adding the mixture to the raw materials of polyunsaturated fatty acids slowly, and carrying out an esterification reaction under certain conditions to obtain glyceride type polyunsaturated fatty acids, wherein the basic catalyst is a lower aliphatic alcohol sodium/potassium or a solution thereof. The preparation method has the following advantages: the procedure of the process is simple, has mild reaction conditions, short reaction time, high yield and good quality of the obtained products.

IPC Classes  ?

• C07C 69/587 - Monocarboxylic acid esters having at least two carbon-to-carbon double bonds
• C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
• C07C 67/03 - Preparation of carboxylic acid esters by reacting an ester group with a hydroxy group

Abstract

Disclosed is a method for recycling urea in the process of separating and purifying unsaturated substances through a urea adduction method. The method comprises the following steps: liposoluble substances containing target unsaturated components are used as raw materials, and subjected to urea adduction, crystallization and filtration to give a filtrate, from which the specific unsaturated components are obtained; the urea adduct is dissolved in a polar solvent, and after the adducted adducts are layered and released, adding a certain solvent to the urea solution to adjust the polarity, then cooling for crystallization, and recycling the urea. The method can realize complete release of the adducted components and recycling and reuse of urea, and the process is simple, the recovery rate is high, and the adduction effect is not influenced when recycling urea for reuse, and the production cost of the urea adduct is reduced, thus alleviating the adverse impact of urea discharges on the environment.

IPC Classes  ?

• C07C 27/02 - Saponification of organic acid esters
• C07C 57/12 - Straight chain carboxylic acids containing eighteen carbon atoms
• C11C 3/00 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis

Abstract

The present invention relates to a preparation method for a polyunsaturated fatty acid-calcium, primarily comprising directly reacting a polyunsaturated fatty acid material and a water-soluble calcium compound to obtain a polyunsaturated fatty acid-calcium salt. The present invention has a simple technical process, short reaction time, and high reaction yield. The produced polyunsaturated fatty acid-calcium product is of high quality, and relatively less byproducts and waste water are produced. The technique is overall environmentally friendly and has small safety risks, and is suitable for scaled production.

IPC Classes  ?

• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
• C07C 57/03 - Monocarboxylic acids
• C07C 57/12 - Straight chain carboxylic acids containing eighteen carbon atoms

Abstract

Provided is a method for preparing a high-content conjugated linoleic acid product by using ordinary vegetable oil as a raw material. The method comprises three steps of alcoholysis, purification and isomerization of the vegetable oil. The alcoholysis of the vegetable oil comprises preparing corresponding methyl ester or ethyl ester by using glyceride as a raw material; the purification of the methyl ester or ethyl ester comprises performing silvered silica gel column chromatography to obtain methyl linoleate or ethyl linoleate having the content higher than 85%; and the purified methyl linoleate or ethyl linoleate is subjected to alkali-catalyzed conjugation to obtain high-content conjugated linoleic acid, and then, conjugated linoleic acid series products can be prepared according to actual needs. The method addresses the situation that high-content conjugated linoleic acid has been prepared based solely on safflower oil before, broadens the source channel of conjugated linoleic acid, and meanwhile provides a process of efficiently separating and purifying linoleic acid; the obtained conjugated linoleic acid has high purity and meets the requirements for application in industries such as pharmaceuticals and health care products.

IPC Classes  ?

• C07C 57/12 - Straight chain carboxylic acids containing eighteen carbon atoms
• C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
• C11C 3/10 - Ester interchange

Abstract

A fixed bed decolorization process for an unsaturated fatty acid, comprising: a polyunsaturated fatty acid or a polyunsaturated fatty acid solution is either passed directly through a fixed bed filler or circulated in the fixed bed filler, a colorless or light-colored polyunsaturated fatty acid product is ultimately produced, at the same time, other than the color, other qualities of the polyunsaturated fatty acid remain unaffected. The decolorization process allows continuous operation or intermittent operation. The fixed bed filler comprises one or a mixture of several among activated carbon, diatomaceous earth, white clay, silicone, and an ion-exchange resin. A top or a middle or a bottom or a combination thereof is employed to feed a polyunsaturated fatty acid feedstock or a polyunsaturated fatty acid feed solution. The filler in the fixed bed can be used repeatedly. The filler can be reused after being washed when decolorization effects thereof become deteriorated or ineffective.

IPC Classes  ?

• C11B 3/00 - Refining fats or fatty oils

Abstract

5 is the same as that of the specification. The glycopeptide compound of the present invention has in-vitro antibacterial activity and has important significance for development of new antibacterial agents.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• C07K 11/00 - Depsipeptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof
• C07K 14/00 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• C07K 11/02 - Depsipeptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof cyclic, e.g. valinomycins
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

The present invention provides a composition for improving macular pigment optical density and preventing or treating age-related macular optical degeneration. The composition comprises lutein, zeaxanthin and tea extracts, wherein the weight ratio of zeaxanthin to lutein is more than or equal to 1. The composition may prevent formation of choroidal neovascularization to achieve effects on comprehensively preventing or treating age-related macular optical degeneration (AMD).

IPC Classes  ?

• A61K 36/82 - Theaceae (Tea family), e.g. camellia
• A61K 36/185 - Magnoliopsida (dicotyledons)
• A61K 31/047 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• A61K 31/07 - Retinol compounds, e.g. vitamin A
• A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• A61K 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61K 33/04 - Sulfur, selenium or telluriumCompounds thereof
• A61K 33/00 - Medicinal preparations containing inorganic active ingredients
• A61K 33/34 - CopperCompounds thereof
• A61K 31/05 - Phenols
• A61K 31/015 - Hydrocarbons carbocyclic

Abstract

Provided is a separation and purification method for vancomycin hydrochloride of a high purity. The method comprises the following steps: (1) obtaining a vancomycin hydrochloride solution from a crude vancomycin product by ion exchange chromatography and obtaining a concentrate by nanofiltration desalination and concentration; (2) adjusting the concentrate with a hydrochloric acid solution and then performing a column chromatography using a reverse chromatography column for the adjusted concentrate; (3) collecting the chromatographic solution of vancomycin to obtain a mixed chromatographic solution; (4) adjusting the mixed chromatographic solution, and separating the solution and the salts by nanofiltration desalination and concentration to obtain a concentrate; and (5) obtaining a vancomycin dry powder with a chromatographic purity of up to 99% and a pure white appearance by dehydrating and drying the concentrate of step (4), or by solvent crystallization or salting-out crystallization.

IPC Classes  ?

• A61K 38/14 - Peptides containing saccharide radicalsDerivatives thereof
• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes

Abstract

A high-content carotenoid compound from adonis amurensis. The content of the total carotenoid of the carotenoid compound is higher than 95%. The content of all-trans (3S, 3'S)-carotenoid is higher than 80%. The carotenoid crystals have a high purity, and can be used in multiple forms in the fields of a dietary supplement of a human being, a food additive, a feed additive and a cosmetic product. In addition, the present invention also provides a method for manufacturing the compound.

IPC Classes  ?

• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene
• A23L 1/30 - containing additives (A23L 1/308 takes precedence);;
• A23K 1/16 - supplemented with accessory food factors; Salt blocks

Abstract

The present invention provides a method for preparing an intermediate compound of sitagliptin represented by formula I. The preparation method comprises: dissolving a compound represented by formula II into an organic solvent; and under the catalysis of fatty acid and effect of chlorosilane, performing a reduction reaction of carbon-carbon double bonds, so as to obtain the intermediate compound of sitagliptin represented by formula I, R being methyl or formoxyl. Te preparation method of the present invention avoids precious metal as a catalyst, and accordingly, the cost is low, the post-treatment is simple, the product has a high yield, chemical purity and optical purity, and de% is greater than 99.6%, and the preparation method can be used in synthesis of sitagliptin and is suitable for industrial production.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

Provided are a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, of low toxicity, high anticancer activity and good stability.

IPC Classes  ?

• C07D 473/16 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/52 - Purines, e.g. adenine
• A61P 35/00 - Antineoplastic agents

Abstract

Provided in the present invention is a method for synthesizing 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde. The synthesis method comprises the following steps: (1) adding acetaldehyde diethyl acetal and ethyl-(1-propenyl)-ether under the effect of a catalyst to produce 1,1,3-triethoxy-2-methyl-butane; (2) pyrolysis synthesizing 1,1,3-triethoxy-2-methyl-butane under the catalytic effects of isoquinoline and p-Toluenesulfonic acid to produce 1-methoxy-2-methyl-1,3-butadiene; (3) dissolving 1-methoxy-2-methyl-1,3-butadiene in anhydrous ethanol solvent for synthesis with a phase transfer catalyst, cetyl-trimethyl ammonium bromide, and a chlorinating agent, trichloroisocyanuric acid, to generate 4,4-diethoxy-3-methyl-1-chloro-butene; (4) combining 4,4-diethoxy-3-methyl-1-chloro-butene with a triphenylphosphine salt to produce a phosphonium salt; and (5) condensing the phosphonium salt under the effects of hydrogen peroxide in conjunction with sodium carbonate solution to generate 1,1,8,8-tetramethyl-2,7-dimethyl-2,4,6-octatriene; then hydrolyzing under acidic conditions to synthesize 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde. The present invention has a simple process route, is easy to operate, and has mild conditions, great yield, and great industrial value.

IPC Classes  ?

• C07C 45/42 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by hydrolysis
• C07C 45/52 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by pyrolysis, rearrangement or decomposition by dehydration and rearrangement involving two hydroxy groups in the same molecule
• C07C 1/32 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from compounds containing hetero atoms other than, or in addition to, oxygen or halogen
• C07C 41/06 - Preparation of ethers by addition of compounds to unsaturated compounds by addition of organic compounds only
• C07C 41/18 - Preparation of ethers by reactions not forming ether-oxygen bonds
• C07C 41/22 - Preparation of ethers by reactions not forming ether-oxygen bonds by introduction of halogenPreparation of ethers by reactions not forming ether-oxygen bonds by substitution of halogen atoms by other halogen atoms
• C07F 9/38 - Phosphonic acids [R—P(:O)(OH)2]Thiophosphonic acids

Abstract

Disclosed is a preparation method of the lycopene intermediate 3-methyl-4,4-dialkoxy-1-butaldehyde. The preparation method comprises the following steps: (1) reacting 2-methyl-3,3-dialkoxy-1-halopropane with magnesium powder in the solvent of anhydrous tetrahydrofuran at a temperature of 45˜65° C. to generate a mixture of Grignard reagents under the protection of an inert gas; and (2) adding N,N-disubstituted carboxamide to the mixture of Grignard reagents and reacting at a temperature of 10° C.˜35° C. to obtain 3-methyl-4,4-dialkoxy-1-butaldehyde. The process route of the present invention is simple and direct, the operation is easy, the conditions are mild and the yield is good, and thus the invention has commercial value.

IPC Classes  ?

• C07C 45/00 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds
• C07C 45/30 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by oxidation with halogen containing compounds, e.g. hypohalogenation
• C07C 41/22 - Preparation of ethers by reactions not forming ether-oxygen bonds by introduction of halogenPreparation of ethers by reactions not forming ether-oxygen bonds by substitution of halogen atoms by other halogen atoms

Abstract

The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R′ and R″ are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.

IPC Classes  ?

• C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
• A61K 31/4245 - Oxadiazoles
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

Abstract

The present invention describes a reduction type coenzyme Q10 powder, a composition thereof, and a preparation method thereof. The reduction type coenzyme Q10 powder is obtained by reacting an oxidation type coenzyme Q10 with the presence of a reducing agent, removing an organic solvent and other purities from a reaction solution after the reaction is finished to obtain an oil-soluble reduction type coenzyme Q10 liquid, and then directly performing prill formation with cold wind on an obtained reduction type coenzyme Q10 greasy substance. The obtained reduction type coenzyme Q10 powder has a lower crystallinity, and in a Cu-Kα X-ray diffraction spectrum, has a strong peak at a diffraction angle 2θ being 18.9°, and has a very strong absorption peak at a diffraction angle 2θ being 22.8°. The reduction type coenzyme Q10 powder obtained in the present invention is in an incompletely crystallized state, has desirable stability and desirable oral bioavailability, and is suitable for use in applications such as dietary supplements, cosmetics or pharmaceuticals.

IPC Classes  ?

• C07C 43/23 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
• C07C 41/26 - Preparation of ethers by reactions not forming ether-oxygen bonds by introduction of hydroxy or O-metal groups
• C07C 41/34 - SeparationPurificationStabilisationUse of additives
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A23L 1/30 - containing additives (A23L 1/308 takes precedence);;
• A61P 39/06 - Free radical scavengers or antioxidants
• A61P 37/04 - Immunostimulants

Abstract

The present invention relates to a pharmaceutical composition for treating hepatitis B virus infection comprising crystalline entecavir as the pharmaceutically active ingredient and one or more pharmaceutically acceptable excipients. The tablet and capsule of the pharmaceutical composition have improved stability compared to that of amorphous entecavir under the conditions of light, high temperature and high humidity.

IPC Classes  ?

• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine

Abstract

Blakeslea trispora strains onto a PDA culture medium so as to obtain a spore suspension; b) propagating spores in a seeding tank so as to obtain seeds for fermentation; c) inoculating the seeds for fermentation onto a fermenter and fermenting said seeds; d) adjusting the fermentation liquid to be basic by using an organic or inorganic base, and filtering so as to obtain wet mycelia; e) treating the wet mycelia with a hydrophobic non-polar organic solvent; f) mixing the wet mycelia with an organic solvent of ester and obtaining a concentrated solution by extracting; g) adding a saturated monohydric alcohol into the concentrated solution, and filtering and crystallizing so as to obtain pure ss-carotene. The content of the ss-carotene in the present invention exceeds 96%, and the yield is above 85%.

IPC Classes  ?

• C07C 1/00 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon
• C12P 23/00 - Preparation of compounds containing a cyclohexene ring having an unsaturated side chain containing at least ten carbon atoms bound by conjugated double bonds, e.g. carotenes
• A23L 1/303 - Vitamins A or D
• A23L 1/275 - Addition of dyes or pigments with or without optical brighteners
• A61K 31/015 - Hydrocarbons carbocyclic

Abstract

The present invention provides a glycopeptide compound or a pharmaceutical salt thereof, as shown in Formula (I) or (II), and a method for preparing same, and pharmaceutical compositions and applications thereof. The glycopeptide compound of the present invention has in-vitro antibacterial activity.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof

Abstract

Disclosed is a composition used for improving the macular pigment density in eyes and preventing or treating age-related macular degeneration (AMD), said composition comprising xanthophyll, zeaxanthin, and tea extract, the ratio of the zeaxanthin to the xanthophyll being greater than or equal to 1.

IPC Classes  ?

• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61K 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• A61K 31/07 - Retinol compounds, e.g. vitamin A
• A61K 31/047 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
• A61K 33/34 - CopperCompounds thereof
• A61K 33/30 - ZincCompounds thereof
• A61K 33/04 - Sulfur, selenium or telluriumCompounds thereof
• A61P 27/02 - Ophthalmic agents

Abstract

A carotenoid oil suspension and preparation method thereof are provided. The method includes the following steps: a) mixing carotenoid with organic solvent, heating the mixture to dissolve the carotenoid sufficiently to obtain carotenoid solution; b) introducing the carotenoid solution obtained in step a) into a vegetable oil solution stirred in high speed by spraying, meanwhile recovering the organic solvent generated during spraying under vacuum condition, then, simultaneously completing recycling and spraying, thereafter, obtaining carotenoid oil suspension; wherein, the carotenoid oil suspension comprises a carotenoid crystal with an average particle size of less than 5 μm. The method is applicable in industrial scale with continuous operation and increased efficiency without additional carotenoid crystal grinding processes, and decreases the degradation of carotenoid during the preparation process of carotenoid oil suspension.

IPC Classes  ?

• A23D 9/007 - Other edible oils or fats, e.g. shortenings or cooking oils characterised by ingredients other than fatty acid triglycerides
• A61K 9/10 - DispersionsEmulsions
• A61K 31/015 - Hydrocarbons carbocyclic
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A23K 20/179 - Colouring agents, e.g. pigmenting or dyeing agents
• A23K 20/158 - Fatty acidsFatsProducts containing oils or fats

Abstract

A method for preparing high level of zeaxanthin is disclosed. The methods known in the prior art have the following disadvantages, for example, using toxic organic solvent, requiring multi-step crystallization process, having long reaction time, high temperature, relatively low yield and being unsuitable for industrial production. In the present invention, oflutein crystal or its fatty acid ester are used as raw material to obtain zeaxanthin through isomerization reaction, which is characterized in using a mixed catalyst consisting of organic alkali catalyst and co-catalyst, wherein the co-catalyst is palladium carbon. The invention has simple process route, low reaction temperature, short reaction duration, high purity and yield and is suitable for industrial production. The product according to the invention has no residual toxic and harmful organic solvent and is suitable for using as food additives or medicine.

IPC Classes  ?

• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene
• B01J 31/02 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides

Abstract

The present invention relates to 2,6,10-trimethyl-3,5,9-undecatrienyl-1-aldehyde represented by formula (3), and a method for preparing this intermediate. The process route of the present invention is simple, the starting materials are available easily, and the cost is low.

IPC Classes  ?

• C07C 45/00 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds

Abstract

The present invention relates to an intermediate (12) of lycopene of 2,6,10-trimethyl-1,1-dialkoxyl-3,5,9-undecantriene of formula, (12) and its intermediate of 4-methyl-5,5-dialkoxyl-1-pentenyl-1-phosphonic acid dialkyl ester of formula (10), and their preparation methods. The process route is simple, the starting materials are available easily, the cost is low, and it is valuable in industry.

IPC Classes  ?

• C07C 43/303 - Compounds having groups having acetal carbon atoms bound to acyclic carbon atoms
• C07F 9/40 - Esters thereof
• C07B 47/00 - Formation or introduction of functional groups not provided for in groups
• C07C 41/50 - Preparation of compounds having groups by reactions producing groups
• C07C 41/48 - Preparation of compounds having groups

Abstract

Disclosed is a preparation method of the lycopene intermediate 3-methyl-4,4-dialkoxy-1-butaldehyd. The preparation method comprises the following steps: (1) reacting 2-methyl-3,3-dialkoxy-1-halopropane with magnesium powder in the solvent of anhydrous tetrahydrofuran at a temperature of 45°C-65°C to generate a mixture of Grignard reagents under the protection of an inert gas; and (2) adding Ν,Ν-disubstituted carboxamide to the mixture of Grignard reagents and reacting at a temperature of 10°C-35°C to obtain 3-methyl-4,4-dialkoxy-1-butaldehyde. The process route of the present invention is simple and direct, the operation is easy, the conditions are mild and the yield is good, and thus the invention has commercial value.

IPC Classes  ?

• C07C 45/00 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds
• C07C 47/198 - Saturated compounds having —CHO groups bound to acyclic carbon atoms or to hydrogen containing ether groups, groups, groups, or groups

Abstract

Provided in the present invention is a method for synthesizing 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde. The synthesis method comprises the following steps: (1) adding acetaldehyde diethyl acetal and ethyl-(1-propenyl)-ether under the effect of a catalyst to acquire 1,1,3-triethoxy-2-methyl-butane; (2) pyrolysis synthesizing 1,1,3-triethoxy-2-methyl-butane under the catalytic effects of isoquinoline and p-Toluenesulfonic acid to acquire 1-methoxy-2-methyl-1,3-butadiene; (3) dissolving 1-methoxy-2-methyl-1,3-butadiene in anhydrous ethanol solvent for synthesis with a phase transfer catalyst, cetyl-trimethyl ammonium bromide, and a chlorinating agent, trichloroisocyanuric acid, to generate 4,4-diethoxy-3-methyl-1-chloro-butene; (4) combining 4,4-diethoxy-3-methyl-1-chloro-butene with a triphenylphosphine salt to acquire a phosphonium salt; and (5) condensing the phosphonium salt under the effects of hydrogen peroxide in conjunction with sodium carbonate solution to generate 1,1,8,8-tetramethyl-2,7-dimethyl-2,4,6-octatriene; then hydrolyzing under acidic conditions to synthesize 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde. The present invention has a simple process route, is easy to operate, and has mild conditions, great yield, and great industrial value.

IPC Classes  ?

• C07C 45/52 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by pyrolysis, rearrangement or decomposition by dehydration and rearrangement involving two hydroxy groups in the same molecule
• C07C 47/21 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation

Abstract

Provided in the present invention is a preparation method for a phosphonic salt, comprising the step of: reacting 3,7,11-trimethyldodec-1,4,6,10-tetraene-3-ol with triarylphosphine and an acid in an alcohol solvent at 50-100°C to form the phosphonic salt, wherein the acid is a sulfamic acid or methanesulfonic acid, and the alcohol solvent is a straight chain monohydric alcohol containing 1-5 carbon atoms. The method is performed in nearly neutral conditions, greatly reducing the generation of impurities greatly and obtaining phosphonic salt with an increased E content. The yield of lycopene obtained by using the phosphonic salt as a raw material is high.

IPC Classes  ?

• C07F 9/54 - Quaternary phosphonium compounds

Abstract

Provided in the present invention are an unsaturated 5-membered benzo-heterocyclic compound with the structure as shown in general formula I or pharmaceutical salts thereof, and a preparation method, a pharmaceutical composition and the use thereof. Experiments have shown that the compound of the present invention has the effects of upregulating the expression activity of bone morphogenetic protein BMP-2 and anti-osteoporosis in vivo, and also has the effect of improving SAMP6 mice osteoporosis symptoms. Activity tests in vitro have shown that the compound of the present invention shows an obvious upregulation effect on bone morphogenetic protein BMP-2.

IPC Classes  ?

• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 493/04 - Ortho-condensed systems
• C07D 495/04 - Ortho-condensed systems
• C07F 9/40 - Esters thereof
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

Abstract

Provided are an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or a pharmaceutically acceptable salt thereof, a preparation method, and a pharmaceutical composition and use thereof, wherein R is CH3 or CF3; R' and R'' are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, bis-substituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, bis-substituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, bis-substituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.

IPC Classes  ?

• C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/4245 - Oxadiazoles
• A61K 31/425 - Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline

Abstract

Provided in the present invention are an oxazole compound with the anti-coxsackie virus structure as shown in formula (I), or pharmaceutically acceptable salts and a preparation method, a pharmaceutical composition and the use thereof, wherein R is CH3 or CF3; R' and R" are H, alkyl or halogen; A is O, S; n is 1 to 9; B is substituted or unsubstituted triazolyl, substituted or unsubstituted dihydro-imidazolinyl, substituted or unsubstituted dihydro-oxazolyl, substituted or unsubstituted dihydro-thiazolyl, substituted or unsubstituted thiadiazolyl, substituted or unsubstituted oxadiazolyl, and substituted or unsubstituted pyrimidinyl. In comparison with the prior art, the oxazole compound of the present invention has an excellent anti-coxsackie virus activity, while having a lower toxicity and a higher safety level.

IPC Classes  ?

• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/4245 - Oxadiazoles
• A61K 31/425 - Thiazoles
• A61K 31/433 - Thiadiazoles
• A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline

Abstract

The invention discloses an intermediate 1-methoxyl-2,6,10-trimethyl-1,3,5, 9-undec-tetraene, and a preparation method and uses thereof. In the synthesis method for the current lycopene intermediate 2-pos double bond C-14 aldehyde (2,6,10-trimethyl-2,5,9-undecatriene-1-aldehyde), expensive methyl iodide, polluting dimethyl sulphide and dangerous strong base are needed, so that the method is hardly applied to industrial production. The invention provides a new compound 1-methoxyl-2,6,10-trimethyl-1,3,5,9-undec-tetraene, and pure 2-pos double bond C-14 aldehyde can be prepared by hydrolyzing and refining the compound. The synthetic route is simplified and the great suitability for industrial production is achieved.

IPC Classes  ?

• C07C 45/42 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by hydrolysis
• C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
• C07C 43/15 - Unsaturated ethers containing only non-aromatic carbon-to-carbon double bonds

Abstract

The invention relates to a novel important lycopene intermediate 3,7,11-trimethyl-1,3,6,10-tetraene-dodecyl diethyl phosphonate. A current lycopene intermediate 2,4,6,10-tetra-double bond pentadec-carbon phosphonate is difficult to synthesize. The invention provides a novel intermediate, which has the following synthesis steps of: preparing 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde from pseudoionone; preparing 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde from the 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde; and subjecting the 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde and tetraethyl methylenediphosphonate to condensation reaction to obtain target product. The invention can generate novel intermediate from raw material pseudoionone only by four reactions, thus the reactions are easy to control and great industrial value are achieved.

IPC Classes  ?

• C07F 9/40 - Esters thereof

Abstract

The present invention relates to a method for preparing a carotenoid oil suspension with low viscosity and high fluidity. The method includes the steps of mixing carotenoid crystals with tetrahydrofuran, heating the resulting mixture to a reflux temperature of about 50˜70° C. under stirring, and filtering-the resulting solution to remove fat-soluble fibers. The resulting filtrate is then condensed to dryness, mixed with a ketone solvent, heated to a reflux temperature of about 60˜80° C., and filtered to remove non-soluble phospholipids. The filtrate obtained is condensed to a residue, and absolute alcohol is added to the residue, and then crystallized under stirring at room temperature. The resulting crystals are filtered and dried to-provide carotenoid crystals. The carotenoid crystals are ground and mixed with plant oils to provide a carotenoid oil suspension with low viscosity and high fluidity, which provides easy filling, for example, into capsules.

IPC Classes  ?

• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin

Abstract

Provided are a method for producing and purifying β-carotene by Blakeslea trispora fermentation and use thereof. The method comprises the following steps: a) separately inoculating the Blakeslea trispora strains onto a PDA culture medium so as to obtain a spore suspension; b) propagating spores in a seeding tank so as to obtain seeds for fermentation; c) inoculating the seeds for fermentation onto a fermenter and fermenting said seeds; d) by using an organic or inorganic base, adjusting the fermentation liquid to be basic, and filtering so as to obtain wet mycelia; e) treating the wet mycelia with a hydrophobic non-polar organic solvent; f) mixing the wet mycelia with an organic solvent of ester and obtaining a concentrated solution by extracting; g) adding a saturated monohydric alcohol into the concentrated solution, and filtering and crystallizing so as to obtain pure β-carotene. The content of the β-carotene in the present invention exceeds 96%, and the yield is above 81%.

IPC Classes  ?

• C12P 23/00 - Preparation of compounds containing a cyclohexene ring having an unsaturated side chain containing at least ten carbon atoms bound by conjugated double bonds, e.g. carotenes
• A23L 1/303 - Vitamins A or D
• A61K 31/07 - Retinol compounds, e.g. vitamin A
• A61K 8/67 - Vitamins
• A61P 3/02 - Nutrients, e.g. vitamins, minerals
• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene
• C12N 1/14 - Fungi Culture media therefor
• C12R 1/645 - Fungi

Abstract

The invention makes public a method for preparing xanthophyll crystals with higher content of zeaxanthin from plant oleoresin. The current methods generally are to get quite pure crystal forms of xanthophyll or zeaxanthin, and they refer to several separation steps. The invention mixes the xanthophyll diester-containing plant oleoresins and food grade alcohol solvents to form smooth solution, and then soap-dissolve the solution under an alkaline environment; then replenish organic solvents and emulsifiers into the reaction solution and drop some alkali solution into the solution to make partial xanthophyll crystals be transformed to be zeaxanthin through epimerization reaction; after the reaction is finished, add the mixed solvents of alcohol solvent and water to separate out the crystals; use the method of centrifugation or filtration to get the crystals; wash the crystals several times with the mixed solution of deionized water and alcohols to remove the impurities among the crystals; recrystallize the gained crystals with absolute ethyl alcohol, and then dry the crystals to get the products. The invention can gain mixture of crystals that contain xanthophyll and zeaxanthin at one time in quite high collection rate.

IPC Classes  ?

• C07C 27/02 - Saponification of organic acid esters
• C07C 29/09 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by hydrolysis
• C07C 29/56 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by isomerisation
• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene
• C09B 61/00 - Dyes of natural origin prepared from natural sources

Abstract

Provided are a linezolid intermediate and the preparation method thereof and a method for synthesizing linezolid. The structure of the intermediate is shown as formula F2, wherein the compound is prepared by a condensation reaction of (S)-N-(3-chloro-2-hydroxy-1-propyl)acetamide and the compound shown in formula F4. In the preparation methods of the compound shown in formula F2 and linezolid, the reaction system is mild, side reactions are few and the product yield is high.

IPC Classes  ?

• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07D 263/20 - Oxygen atoms attached in position 2

Abstract

A carotenoid oil suspension and preparation method thereof are provided. Said method includes the following steps: a) mixing carotenoid with organic solvent, heating the mixture to dissolve the carotenoid sufficiently to obtain carotenoid solution; b) introducing the carotenoid solution obtained in step a) into a vegetable oil solution stirred in high speed by spraying, meanwhile recycling the organic solvent generated during spraying under vacuum condition, then, simultaneously completing recycling and spraying, thereafter, obtaining carotenoid oil suspension; wherein, said carotenoid oil suspension comprises a carotenoid crystal with an average particle size of less than 5μm. Said method is applicable in industrial scale with continuous operation and increased efficiency without additional carotenoid crystal grinding processes, and decreases the degradation of carotenoid during the preparation process of carotenoid oil suspension.

IPC Classes  ?

• A61K 9/10 - DispersionsEmulsions
• A61K 31/01 - Hydrocarbons
• A61K 31/015 - Hydrocarbons carbocyclic

Abstract

Disclosed is an intermediate of lycopene, 2,6,10-trimethyl-3,5,9-undecatrien-1-carboxaldehyde represented by formula (3), and a method for preparing this intermediate. The process route is simple, the starting materials are available easily, and the cost is low.

IPC Classes  ?

• C07C 45/42 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by hydrolysis
• C07C 45/45 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by condensation
• C07C 47/21 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation

Abstract

Disclosed are an intermediate (12) of lycopene, 2,6,10-trimethyl-1,1-bialkoxyl-3,5,9-undecan-triene, and the intermediate (10) thereof, 4-methyl-5,5-bialkoxyl-1-penten- 1-phosphonic acid bialkyl ester, and their preparation methods.. The process route is simple, the starting materials are available easily, the cost is low, and it is valuable in industry.

IPC Classes  ?

• C07C 43/03 - Ethers having all ether-oxygen atoms bound to acyclic carbon atoms
• C07C 41/48 - Preparation of compounds having groups
• C07F 9/28 - Phosphorus compounds with one or more P—C bonds
• C07B 47/00 - Formation or introduction of functional groups not provided for in groups

Abstract

12 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom. The derivatives of the present invention have the functions of antiviral medicine.

IPC Classes  ?

• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• C07D 235/04 - BenzimidazolesHydrogenated benzimidazoles
• C07D 333/10 - Thiophene
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 487/04 - Ortho-condensed systems
• C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 235/26 - Oxygen atoms
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

Disclosed is an intermediate 1-methoxyl-2,6,10-trimethyl-1,3,5,9- undec-tetraene and a preparation method and uses thereof. The synthesis method of the current lycopene intermediate 2-position double bond C-14 aldehyde (2,6,10-trimethyl-2,5,9-undec-triene-1-aldehyde) needs expensive methyl iodide, polluting dimethyl sulphide and dangerous strong base so that the current lycopene intermediate is difficult to apply to industrial production. Provided is a new compound which is 1-methoxyl-2,6,10-trimethyl-1,3,5,9- undec-tetraene, and pure 2-position double bond C-14 aldehyde can be prepared by hydrolyzing and refining the compound. The method simplifies the synthetic route and is suitable for industrial production.

IPC Classes  ?

• C07C 43/16 - Vinyl ethers
• C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
• C07C 47/21 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
• C07C 45/42 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by hydrolysis

Abstract

A lycopene intermediate 3, 7, 11-trimethyl-1, 3, 6, 10-tetraene-dodecyl diethyl phosphonate is disclosed. The preparation method thereof is as follows: preparing 2, 6, 10-trimethyl-3, 5, 9-undecane triene-1-aldehyde from pseudo ionone; then preparing 2, 6, 10-trimethyl-2, 5, 9-undecane triene-1-aldehyde; condensing 2, 6, 10-trimethyl-2, 5, 9-undecane triene-1-aldehyde with tetra-ethyl methylene diphosphonate to obtain the target product. The reaction in this invention is easy to control, and the invention has great industrial values.

IPC Classes  ?

• C07F 9/40 - Esters thereof
• C07C 11/21 - AlkatrienesAlkatetraenesOther alkapolyenes
• C07C 1/34 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from compounds containing hetero atoms other than, or in addition to, oxygen or halogen reacting phosphines with aldehydes or ketones, e.g. Wittig reaction

Abstract

1, 4, 6, 10-tetra-double bond pentadec-carbon phosphonate of formula (4), and preparation method thereof are provided. The preparation method comprises: reacting a pseudo ionone of formula (2) with sulfonium salt to prepare a epoxide of formula (9), and then reacting the epoxide of formula (9) with magnesium bromide to prepare a C-14 aldehyde of formula (3); condensing the C-14 aldehyde of formula (3) with tetra-alkyl methylene diphosphonate to obtain 1, 4, 6, 10-tetra-double bond pentadec-carbon phosphonate of formula (4). Furthermore, the preparation method of lycopene via 1, 4, 6, 10-tetra-double bond pentadec-carbon phosphonate of formula (4) is also provided. The present method has the advantages of short route, easily obtained raw materials, and low cost.

IPC Classes  ?

• C07F 9/40 - Esters thereof
• C07C 11/21 - AlkatrienesAlkatetraenesOther alkapolyenes
• C07C 1/34 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from compounds containing hetero atoms other than, or in addition to, oxygen or halogen reacting phosphines with aldehydes or ketones, e.g. Wittig reaction

Abstract

A preparing method for xanthophyll crystals with a higher content of zeaxanthin from plant oleoresin is provided. The method includes mixing a xanthophyll diester-containing plant oleoresin and food-grade alcohol solvent to form a homogeneous solution, and saponifying it under alkaline conditions; replenishing organic solvent and emulsifier into the mixed solution and instilling strong alkali solution to make part of the xanthophyll crystals epimerized and changed into zeaxanthin; adding a mixed solvent of alcohol and water to precipitate the crystals; centrifuging or filtering to obtain crystals; washing the crystals for several times with a mixed solution of deionized water and alcohol to eliminate impurities; recrystallizing the obtained crystals with dry ethanol and drying. The crystals containing xanthophyll and zeaxanthin can be obtained at a higher yield through the present method.

IPC Classes  ?

• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene

Abstract

10 from reductases.

IPC Classes  ?

• C12P 7/66 - Preparation of oxygen-containing organic compounds containing the quinoid structure

Abstract

The present invention relates to thienopyridazine compounds of formula (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 are independently H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6-membered ring containing N, S or O, or its optical isomers, R4 is a halophenyl monosubstituted or disubstituted at any position. The present invention provides the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer.

IPC Classes  ?

• A01N 43/58 - 1,2-DiazinesHydrogenated 1,2-diazines
• A01N 43/60 - 1,4-DiazinesHydrogenated 1,4-diazines
• A61K 31/50 - PyridazinesHydrogenated pyridazines
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• C07D 237/26 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
• C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
• C07D 237/28 - Cinnolines
• C07D 495/04 - Ortho-condensed systems

Abstract

A compound of formula (I), the preparation methods and use thereof are disclosed. The compound is obtained by fermenting the mutant strain of Amycolatopsis orientalis CGMCC NO: 3053, wherein the bond of the 4-hydroxy of the saccharide group on benzyl hydroxyl of 6-amino acid on the peptide backbone is an axial bond. The compound has a good antibacterial activity and can be used in preparing antibacterial agent.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61P 31/04 - Antibacterial agents
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12R 1/01 - Bacteria or actinomycetales

Abstract

A method for preparing d-biotin is disclosed, which comprises condensing (3aR,8aS,8bS)-1,3-dibenzyl-2-oxo-decahydroimidazo[3,4-d]thieno[1,2-a]sulfonium halide with trialkyl methanetricarboxylate in the presence of base to give （3aS, 4S, 6aR）-1,3- dibenzyl -4-(ω,ω,ω-tricarbalkoxy-butyl)- tetrahydro -1H- thieno[3,4-d]imidazol-2,4(1H)-one as intermediate, and then subjecting the intermediate to hydrolysis, decarboxylation and ring-closing steps to give d-biotin.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• C07D 235/00 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
• C07D 333/00 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom

Abstract

A preparation method of carotenoid oil suspensions with low viscosity and high fluidity and the use in the manufacture of food, dietary supplement and drug thereof. The method includes mixing carotenoid crystal with tetrahydrofuran, heating the mixture to 50-70 °C under stirring to dissolve the crystal, filtering, condensing to obtain the concentrate; mixing the concentrate with ketone, heating the mixture to 60-800C to dissolve the concentrate, filtering, condensing, adding absolute ethanol at room temperature, crystallizing under stirring, vacuum drying to obtain carotenoid crystal; grinding efficiently the carotenoid crystal and then mixing it with vegetable oils, or mixing the carotenoid crystal with vegetable oils and grinding to obtain carotenoid oil suspensions.

IPC Classes  ?

• A61K 9/10 - DispersionsEmulsions
• A61K 31/01 - Hydrocarbons
• A61K 31/015 - Hydrocarbons carbocyclic
• A23L 1/302 - Vitamins
• A61P 3/02 - Nutrients, e.g. vitamins, minerals

Abstract

The present invention relates to a crystalline form of entecavir and its process for preparation, and provides a pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of entecavir. Furthermore, the present invention also provides a use of the crystalline form of entecavir in preparation for a medicament for the treatment of hepatitis B viral infections. The present invention is beneficial toe preparations for pharmaceutical formulations and enhancements of its bioavailability.

IPC Classes  ?

• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine

Abstract

The present invention provides caffeoylquinic acid derivatives and a method of preparing for the same, and also provides pharmaceutical compositions containing caffeoylquinic acid derivatives, and uses of caffeoylquinic acid derivatives in preparation of a medicament for the treatment or prophylaxis of virus diseases, in particular, uses of respiratory syncytial virus and hepatitis B virus, which has the characteristics of safety, high effectiveness and low toxicity.

IPC Classes  ?

• C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
• C07C 235/40 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton

Abstract

Thienopyridazine compounds of formular (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 is separately H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6- membered ring containing N, S or O, or its optical isomers, R4 is halophenyl monosubstituted or disubstituted at any position. And the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61P 35/00 - Antineoplastic agents

Abstract

A deshydroxy vancomycin compound,a method of its preparation and a pharmaceutical composition comprising a pharmaceutically effective amount of the deshydroxy vancomycin and the use of the said composition in the preparation of drugs for the treatment of susceptible bacteria infections. The method includes the following steps: (1) A concentrated vancomycin solution used to prepare the deshydroxy vancomycin is produced by fermentation of Amycolatopsis orientalis CGMCC No. 1183. (2) An ancomycin hydrochloride straining filtrate comprising the deshydroxy vancomycin is obtained by separating and purifying the concentrated vancomycin solution bycolumn chromatography. And (3) The deshydroxy vancomycin is obtained by separating and purifying the said filtrate by chromatograph. In which, the column chromatography process is processed in a gel chromatographic column comprising salt-water mobile phase; the chromatography process is processed in a macropore polymeric adsorbent chromatographic column comprising buffer-methanol mobile phase.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• C12N 1/20 - BacteriaCulture media therefor
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 35/74 - Bacteria
• A61K 38/14 - Peptides containing saccharide radicalsDerivatives thereof
• A61P 31/04 - Antibacterial agents

Abstract

A carotenoid formulation in oil suspensions, comprises a carotenoid with an average particle size of 10μm or less, an antioxidant and an edible oil. A feed contains the said carotenoid formulation, a method for preparing the feed and use of the carotenoid formulation as an additive of animal feeds, foods, cosmetics and/or pharmaceuticals. The active ingredients in the feed granules are homogeneously distributed in the feed granules, majority of which are substantially distributed inside the granules, to reduce the loss caused by oxidation on the surface.

IPC Classes  ?

• A23K 1/16 - supplemented with accessory food factors; Salt blocks
• A23L 1/275 - Addition of dyes or pigments with or without optical brighteners
• A61K 47/06 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• C07C 403/24 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by six-membered non-aromatic rings, e.g. beta-carotene

Abstract

A pharmaceutical composition for treating hepatitis B virus infection. Said composition comprises crystal entecavir as the active ingredient and pharmaceutically acceptable excipients.

IPC Classes  ?

• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 31/12 - Antivirals

Abstract

The present invention provides 2, 6-dinitrogen-containing substituted purine compounds of formula (A) or their salts or their solvates or the solvates of their salts, as well as pharmaceutical compositions containing such compounds. The compounds of the invention have the characteristic of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.

IPC Classes  ?

• C07D 473/16 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
• C07H 19/16 - Purine radicals
• C07H 19/173 - Purine radicals with 2-deoxyribosyl as the saccharide radical
• C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
• A61K 31/52 - Purines, e.g. adenine
• A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are caffeoyl quinic acid derivatives and preparation method, pharmaceutically composition containing the same and the use thereof for treatment or prophylaxis of virosis, in particular the use for treatment or prophylaxis of respiratory syncytial virus and hepatitis B virus, which has the advantages of security, high effectiveness and low toxicity.

IPC Classes  ?

• C07C 235/40 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
• C07D 207/04 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The present invention discloses a crystalline form of entecavir and its preparation, and provides pharmaceutical compositions comprising a therapeutically effective amount of the crystalline form of entecavir. Furthermore, the invention also provides the use of the crystalline form of entecavir in preparation of a medicament for the treatment of hepatitis B viral infections. The invention is in favor of the preparation of pharmaceutical formulations and the enhancement of its bioavailability.

IPC Classes  ?

• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61P 31/20 - Antivirals for DNA viruses

Abstract

This invention has disclosed a method for preparation of food-grade zeaxanthin through chemical isomerizaton reaction from lutein. The technical issues to be solved in this invention are quite low product yield obtained with existing methods, need of purification treatment process, and inadaptability to industrialized production. The technical schemes of this invention are: a. Mix xanthophyll crystal or its fatty acid ester with food-grade glycol or propylene glycol, for full dissolution under 60-90° C. temperature. Add organic alkali into the mixed liquor acquired from step 1, for isomerization reaction to take place under inertial environment. c. Dilute the reaction solution gained from step b with the mixed solution of deionized water and ethanol, and separate the obtained crystal with conventional separating method. d. Vacuum dries the acquired crystal from step c, to get the zeaxanthin crystal. Glycol or propylene glycol is used in this invention for isomerization reaction under inertial environment after it has fully dissolved raw material under proper temperature. The product yield is reachable to more than 60%, very adaptable to industrialized product, without the need for further purification treatment.

IPC Classes  ?

• C07C 51/353 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by isomerisationPreparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by change of size of the carbon skeleton