abstract |
The invention provides processes by which (R)-3-[4- (trifluoromethyl)phenylamino]pentanamide derivatives useful as intermediates of drugs, particularly, cholesteryl ester transfer protein (CETP) inhibitor can be easily and simply produced from easily available starting materials. According to the invention, (S)-N-[4-(trifluoromethyl)- phenyl]-3-hydroxypentanamide is produced from easily available raw materials and converted into (R)-3-[4-(trifluoromethyl)- phenylamino]pentanamide through (R)-4-ethyl-1-[4-(trifluoro- methyl)phenyl]-2-azetidinone. Further, (R)-3-[4-(trifluoro- methyl)phenylamino]pentanamide derivatives are produced by reacting (R)-4-ethyl-1-[4-trifluoromethyl]phenyl]-2- azetidinone with a carbamic acid ester. |