Process for the preparation of Efinaconazole
AssigneeLupin Limited
InventorsSachin Arun Sasane, Devendrakumar Paramsukh Varma, Rajesh Harishankar Vyas, Nandu Baban Bhise, Girij Pal Singh, Krishnat Hanmant Kumbhar
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Abstract
The present invention provides an improved process for the preparation of Efinaconazole in higher yield by the ring-opening addition reaction of epoxytriazole with 4-methylenepiperidine or its acid addition salt under mild conditions without using a large excess of 4-methylenepiperidine in the presence of an alkali or an alkaline earth metal halide.
Claims3
An improved process for the preparation of Efinaconazole or pharmaceutically acceptable salts thereof comprises reacting (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]oxirane with 4-methylenepiperidine or its acid addition salt in the presence of an alkali or an alkaline earth metal halide.
Dependencies are inferred from the claim text.