A process for preparing the prostaglandin derivatives is provided, wherein the benzoyl and p-nitrobenzoyl groups are used as the hydroxyl protective groups. A pharmaceutical composition comprising the prostaglandin derivatives is also provided.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
C07D 307/00 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
The present invention provides a process for preparation of stable, free flowing, non-hygroscopic crystalline alpha form of Imatinib mesylate. The present invention also provides a pharmaceutical composition using the stable, free flowing, non hygroscopic crystalline alpha form of Imatinib mesylate of the present invention.
C07D 401/14 - 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 three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07C 303/32 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention is directed to solid forms of pterostilbene. Five polymorphs of pterostilbene are disclosed herein. In addition, a t-butanol solvate and an x-ray amorphous form of pterostilbene are further disclosed.
The present invention relates to Stilbene derivatives of the general formula I or a pharmaceutically acceptable salt thereof have properties such as high water solubility, bioavailability and effective as carcinostatics.
C07C 39/215 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic, containing only six-membered aromatic rings as cyclic part, with unsaturation outside the rings with at least one hydroxy group on a non-condensed ring containing the structure, e.g. diethylstilbestrol
C07C 43/215 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring having unsaturation outside the six-membered aromatic rings
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
5.
A KEY INTERMEDIATE FOR THE PREPARATION OF STILBENES
The present invention provides a scalable process for the preparation of Stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4'-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4'-O-tetrahydropyranyl Stilbene (ii) deprotecting the obtained 3,5-Dialkyl- 4'-O-tetrahydropyranylstilbene yields Stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4'-O-tetrahydropyranylstilbene, which is a key intermediate for the synthesis of Stilbenes such as Pterostilbene and Resveratrol.
A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercapto methyl) cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.
The present invention refers to an parenterally administerable aqueous formulation containing paracetamol. For enhancing stability the formulation contains a sulphur containing antioxidant, preferably sodium metabisulfite. For making the formulation more soluble it contains hydroxy propyl beta cyclodextrin. The composition is used as analgesic.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 33/04 - Sulfur, selenium or telluriumCompounds thereof
8.
AN EFFICIENT PROCESS TO INDUCE ENANTIOSELECTIVITY IN PROCARBONYL COMPOUNDS
An efficient method to induce the enantioselectivity in procarbonyl compounds using chiral organometallic complexes. The present invention is also described a method for producing organo metallic complexes using a base and a metal halide.
C07C 215/76 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring
9.
PREPARATION OF ETHYL-3'-[((7-CHLORO-2-QUINOLINYL)ETHENYL)PHENYL]-3-OXOPROPANOATE, A KEY INTERMEDIATE FOR MONTELUKAST SODIUM
A process for preparing β- ketoester of formula (III) comprises; (a)condensing alkyl 3- formylbenzoate with 7-Chloroquinaldine to give alkyl 3-[((7-chloro-2-quinolinyl) ethenyl)] benzoate; and (b) reacting alkyl 3-[((7-chloro-2-quinolinyl) ethenyl)] benzoate with an alkyl ester in presence of metal hydride/metal alkoxides to obtain a compound β- ketoester of structural formula (Ill) or (a) condensing isophthalaldehyde with 7-Chloroquinaldine to give Ethyl 3-[((7-chloro-2- quinolinyl) ethenyl)] benzaldehyde (b) reacting Ethyl 3-[((7-chloro-2-quinolinyl) ethenyl)] benzaldehyde with an α-halo ester in presence of a metal catalyst to give Ethyl 3'-[((7-chloro- 2-quinolinyl) ethenyl)phenyl] -3 -hydroxy propanoate; and (c) treating Ethyl 3'-[((7-chloro-2- quinolinyl)ethenyl)phenyl]-3-hydroxy propanoate with Collins reagent in an organic solvent to obtain a compound β- ketoester of structural formula (III).
A process for synthesizing a β- ketoester of formula (VII) which comprises: (a) converting 3-methylbenzoic acid into alkyl 3-methylbenzoate; (b) reacting 3 -methyl benzoate to form alkyl 3 -bromomethylbenzoate; (c)converting alkyl 3-bromo methyl benzoate into alkyl 3-formylbenzoate; (d) condensing alkyl 3-formyl benzoate with 7- Chioroquinaldine to give alkyl 3- [((7-Chloro-2-quinolinyl) ethenyl)]benzoate; (e) hydrolyzing alkyl 3 -[((7-Chloro-2-quinolinyl)ethenyl) benzoate to give 3-[((7- Chloro- 2-quinolinyl)ethenyl)]benzoic acid; and (f) reacting 3-[((7-Chloro-2-quinolinyI) ethenyjbenzoic acid with a malonate to obtain a compound of structural formula VII.
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