The present invention provides a stable amorphous Tegoprazan of the formula (I). The present invention provides stable amorphous Tegoprazan free from other solid state forms and stable over shelf life and does not convert into any other solid state forms.
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 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
2.
A NOVEL PROCESS FOR THE PREPARATION OF CRYSTALLINE LINEZOLID FORM-III
The invention relates to a novel process for preparation of crystalline Linezolid Form-III. The crystalline Linezolid Form-III obtained by the process is highly pure with HPLC purity equal to or greater than 99.9% with single un-known impurity less than 0.05%.
S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.
The present invention relates to a novel and improved process for the preparation of Sitagliptin of Formula (I) and its pharmaceutically acceptable salts. The present invention also relates to novel intermediates and process for the preparation of intermediates used in the preparation of Sitagliptin.
C07D 487/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains two hetero rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
The invention relates to novel oxazolidinone compound. More particularly, the invention relates to novel [(S)- N- [[3-[4-fluoro-3-morpholino phenyl]-2-oxooxazolidin-5-yl] methyl] acetamide] compound of Formula-I which was disclosed in Indian Patent Application No. 5063/CHE/2013 and corresponding PCT/IN2014/000018. The compound is a broad spectrum antimicrobial agent effective against Multi-Drug Resistant S. Maltophilia pathogen and a large number of gram positive and gram negative pathogens. The compound has shown excellent biological activities against S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
A novel oxazolidinone compound (S)-N-((3-(4-fluoro-3-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide of formula -I and a process for the preparation thereof. Compound-I.
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
C07D 413/10 - 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 carbon chain containing aromatic rings
7.
A PROCESS FOR PREPARATION OF TRANS (LR,2R)-CYCLO HEXANE 1, 2-DICARBOXYLIC ACID
A commercially viable process for industrial preparation of trans-(l R,2R)-cyclohexane 1,2- dicarboxylic acid represented by compound of Formula-I, wherein the compound has more than 99% HPLC purity. The compound of Formula-I is a key intermediate in preparation of Lurasidone hydrochloride which is a well known antipsychotic agent used for treatment of schizophrenia.
C07C 51/02 - Preparation of carboxylic acids or their salts, halides, or anhydrides from salts of carboxylic acids
C07C 51/36 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by hydrogenation of carbon-to-carbon unsaturated bonds
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 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
A commercially viable process for industrial preparation of [(S)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine which is a key intermediate for saxagliptin synthesis and is represented by compound of Formula-VI. The compound-VI obtained by the process of present invention has more than 99.5% HPLC purity, not more than 0.15 % of dihydroxy impurity, not more than 0.05% of isomer impurity and not more than 0.1% of any unknown impurity. Formula (VI).
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
9.
Process for preparation of Linezolid and its novel intermediates
A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.
C07D 263/06 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by oxygen atoms, attached to ring carbon atoms
C07D 263/14 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals substituted by oxygen atoms
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 269/00 - Heterocyclic compounds containing rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms according to more than one of groups
C07D 413/10 - 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 carbon chain containing aromatic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to oxazolidinone antibacterial agent anhydrous Linezolid crystalline Form-II. The anhydrous Linezolid crystalline Form-II of the invention comprises less than 0.5% of water content. The anhydrous Linezolid crystalline Form-II of the invention is characterized by the XRPD spectrum and IR spectrum described in the specification.
A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4- morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.
Disclosed herein is process for preparation of crystalline form of (S)-5-methoxy-2-[[(4- methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazolemagnesium dihydrate which comprises: dissolving (S)-Omeprazole potassium in dimethyl formamide; reacting with magnesium chloride hexa hydrate; removing the salts from the mixture; and precipitating the (S)-Omeprazole magnesium di hydrate crystalline form by adding anti solvent. The anti-solvent used in the above process is selected from the group consisting of ketones such as acetone or methyl isobutyl ketone; esters such as ethyl acetate, and ethers like methyl tertiary butyl ether.
C07D 401/00 - 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
13.
PROCESS FOR PREPARATION OF NOVEL SALT OF VORICONAZOLE OXALATE FORM-C
C07D 403/06 - 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 carbon chain containing only aliphatic carbon atoms
14.
A PROCESS FOR THE PREPARATION OF ANHYDROUS POLYMORPHIC FORM OF OLANZAPINE
Malononitrile is reacted with Propionaldehyde in presence of Sulphur Powder and Triethylamine in N,N-dimethlyformamide to give 5-Amino4- Cyano-2 -Methyl Thiophene. 2-fluoronitrobenzene is condensed with 5- Amino-4-Cyano-2-Methyl Thiophene in Isopropyl alcohol and Potassium Hydroxide powder give 4-cyano-2-methyl-1-(2-nitrophenyl amino) Thiophene. Reduction of 4-cyano-2-methyl-1-(2-nitrophenyl amino) Thiophene with Stannous Chloride and Hydrochloric acid in Isopropyl; Alcohol and followed by cyclization to get 4-Amino-2-Methyl-10H- Thieno ⏧2,3,-b]⏧1,5] Benzodiazepine Condensation of 4-amino-2-methyF10H-Thieno ⏧2,3,-b]⏧1,5] Benzodiazepine and N-methyl Piperazine in presence of Dimethyl Sulphoxide and Toluene gives Olanzapine Technical grade, in anhydrous form. Treatment of anhydrous technical Olanzapine with acetone followed by subsequent precipitation with an anti solvent gave anhydrous OLANZAPINE of Form-II.
Disclosed herein is cost effective and industrially feasible process for the preparation of (+) Clopidogrel bisulfate. The present invention further discloses a novel method of precipitation of (+) Clopidogrel bisulfate Form I directly from solvent mix of methanol and acetone in presence of sulfuric acid at a temperature of 25-40° C
C07C 229/36 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
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