发明名称 |
AN IMPROVED PROCESS FOR THE PREPARATION OF APREPITANT |
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 ≧99.5%. |
申请公布号 |
EP2817305(B1) |
申请公布日期 |
2016.09.28 |
申请号 |
EP20130752547 |
申请日期 |
2013.02.22 |
申请人 |
PIRAMAL ENTERPRISES LIMITED |
发明人 |
LADKAT, PRASHANT;WAGH, GANESH;JAGTAP, ASHUTOSH;ROY, MITA;HARIHARAN, SIVARAMAKRISHNAN;CHOUKEKAR, MILIND |
分类号 |
C07D413/06;A61K31/5377;C07D265/32 |
主分类号 |
C07D413/06 |
代理机构 |
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