期刊
LETTERS IN ORGANIC CHEMISTRY
卷 10, 期 3, 页码 159-163出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1570178611310030003
关键词
Vildagliptin; cost-effective; TCT
资金
- Natural Science Foundation of Chongqing (CSTC) [2006BB5286]
- Chongqing Medical University
A cost-effective synthetic approach to prepare vildagliptin under gentle experimental conditions has been reported with good yield and high purity. It was initiated with L-proline via successful reaction with chloroacetyl chloride in THF (Tetrahydrofuran) to give the 1-(2-chloroacetyl)-pyrrolidine-2-carboxylic acid, which was then treated by TCT (2, 4, 6-trichloro-1, 3, 5-triazine) in DCM (dichloromethane), and converted into 1-(2-chloroacetyl)-pyrrolidine-2-carboxamide, then further converted into 1-(2-chloroacetyl)-pyrrolidine-2-carbonitrile after dehydrated by TCT in DMF (N, N-dimethylformamide), the latter product was reacted with 3-aminoadamantanol to get vildagliptin. The total yield of vildagliptin was about 48%, the purity was about 99%.
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