Patent ID: 9199933
Filing Date: 2015-12-01
Classification: C07C,C07D

Abstract:
1. A process for the preparation of the saxagliptin comprising the steps of: i) reacting the compound of formula Ill or its acid addition salts wherein R and R1 independently is H or C1-C6 substituted or unsubstituted alkyl group; L is a halogen or leaving group; with alkali metal azide in the presence of a phase transfer catalyst to obtain a compound of formula IV or its acid addition salts wherein R and R1 independently is H or C1-C6 substituted or unsubstituted alkyl group; ii) treating the compound of formula IV with chiral reagent to obtain the compound of formula V; iii) hydrolysis of the compound of formula V by employing mineral acid to obtain a compound of formula VI wherein R and R1 independently is H or C1-C6 substituted or unsubstituted alkyl group; iv) reacting the compound of formula VI with the compound 2-azabicyclo[3.1.0]hexane-3-carboxamide of formula VII or its acid addition salts in the presence of a coupling reagent and coupling additives to obtain a compound of formula VIII or its acid addition salts; v) dehydrating the compound of formula VIII or its acid addition salts in the presence of a dehydrating reagent and base to obtain a compound of formula IX or its acid addition salts; vi) reducing the compound of formula IX or its acid addition salts in the presence of a metal catalyst to obtain compound of formula X or its acid addition salts