A Cost-Effective Method to Prepare Pure Vildagliptin

Author(s): Jun Peng, Yue Feng, Zhu Tao, Yingjie Chen, Xiangnan Hu.

Journal Name: Letters in Organic Chemistry

Volume 10 , Issue 3 , 2013

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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%.

Keywords: Vildagliptin, cost-effective, TCT.

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Article Details

Year: 2013
Page: [159 - 163]
Pages: 5
DOI: 10.2174/1570178611310030003
Price: $65

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