Sitagliptin, salts and polymorphs thereof
OwnerDhananjay Govind Sathe, Subhash Vishwanath Damle +4inventors
InventorsDhananjay Govind Sathe, Subhash Vishwanath Damle, Nitin Dnyaneshwar Arote, Rakesh Ramchandra Ambre, Kamlesh Digambar Want, Tushar Anil Naik
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Abstract
The present invention relates to an improved process for preparation of Sitagliptin or pharmaceutically acceptable salts thereof. The present invention further relates to novel polymorphs of Sitagliptin salts and process for preparation thereof.
Claims19
A process for preparation of Sitagliptin or pharmaceutically acceptable salts thereof comprising the steps of,
- a) hydrogenating methyl 4-(2,4,5-trifluorophenyl)-3-oxobutanoate in presence of less than about 0.5% w/w of (S)—BINAP—RuCl2 with respect to methyl 4-(2,4,5-trifluorophenyl)-3-oxobutanoate to obtain 3(S)-4-(2,4,5-trifluorophenyl)-3-hydroxybutanoic acid;
- and
- b) converting said 3(S)-4-(2,4,5-trifluorophenyl)-3-hydroxybutanoic acid to Sitagliptin or pharmaceutically acceptable salts thereof.
A process for preparation of Sitagliptin or pharmaceutically acceptable salts thereof comprising the steps of,
- a) debenzyloxylation of 3(R)-3-[(benzyloxy)amino]-1-[3-(trifluoromethyl)-5H, 6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluoro phenyl)butan-1-one using hydrogen gas in presence of a catalyst and an additive to obtain a reaction mixture, wherein said additive is selected from benzyl chloride, benzyl bromide, benzyl iodide or substituted derivatives thereof;
- b) isolating Sitagliptin from said reaction mixture.
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Dependencies are inferred from the claim text.