AN IMPROVED PROCESS FOR THE PREPARATION OF APREPITANT

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专利权人:

PIRAMAL ENTERPRISES LIMITED

发明人:

LADKAT, PRASHANT,WAGH, GANESH,JAGTAP, ASHUTOSH,ROY, MITA,HARIHARAN, SIVARAMAKRISHNAN,CHOUKEKAR, MILIND

申请号：

EP13752547

公开号：

EP2817305A4

申请日:

2013.02.22

申请国别(地区):

EP

年份:

2015

代理人:

摘要：

The present invention provides a process for the preparation of 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (Aprepitant) comprising condensation of 2-(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(S)-(4-fluorophenyl)morpholine hydrochloride salt with 2-(2-chloro-1-iminoethyl)hydrazinecarboxylic acid methyl ester to obtain the reaction mixture containing 2-[2-[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]-1-iminoethyl]hydrazinecarboxylic acid methyl ester, which is in-situ cyclized in the presence of dimethylsulfoxide and a polar protic solvent at a low temperature to yield aprepitant having purity &gE99.5%.

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