Patent ID: 8846916
Filing Date: 2014-09-30
Classification: A61P,C07B,C07C,C07D

Abstract:
1. A process for the preparation of enantiomerically enriched sitagliptin, or a pharmaceutically acceptable salt thereof, comprising the steps: (i) resolving a racemic β-amino acid, or a derivative thereof, with an acid resolving agent to form an enantiomerically enriched β-amino acid or a derivative thereof; (ii) reacting the enantiomerically enriched β-amino acid or derivative thereof with 3-trifluoromethyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine or a salt thereof; and (iii) isolating enantiomerically enriched sitagliptin; wherein the derivative is an alkyl, alkenyl, alkynyl, aryl or arylalkyl ester.