METHOD FOR PREPARING INTERMEDIATE OF SITAGLIPTIN USING CHIRAL OXIRANE

摘要

PURPOSE: A method for preparing sitagliptin intermediate of sitagliptin is provided to efficiently prepare 3-hydroxy-4-(2,4,5-trifluorophenyl)butyric acids as main intermediates of sitagliptin, especially (3S)-3-hydroxy-4-(2,4,5-trifluorophenyl)butyric acids. CONSTITUTION: A method for preparing 3-hydroxy-4-(2,4,5-trifluorophenyl)butyric acids of chemical formula 1a comprises: performing nitrilization of 4-(2,4,5-trifluorobenzyl)-oxylane of chemical formula 2a in the presence of a catalyst to prepare 4-(2,4,5-trifluorophenyl)-3-hydroxybutane nitrile of chemical formula 3a; and performing hydrolysis of the 4-(2,4,5-trifluorophenyl)-3-hydroxybutane nitrile in the presence of strong base.