| 摘要 |
The present invention describes a process for the preparation of sitagliptin or its pharmaceutically acceptable salts of formula (1) comprising the steps of a) condensation of compound of formula (2), wherein R is amino protecting group with compound of formula (3), which may be used in its free base form or in a form of a salt in the presence of a coupling agent and a basic solvent that is N-methylimidazole to obtain the compound of formula (4), and b) deprotection of compound of formula (4) to obtain sitagliptin base that can be further transformed into its pharmaceutically acceptable salt. The process is cost effective, environmentally friendly, inexpensive and easily scaled up to commercial level. |
