Abstract
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.
Letters in Organic Chemistry
Title:A Cost-Effective Method to Prepare Pure Vildagliptin
Volume: 10 Issue: 3
Author(s): Jun Peng, Yue Feng, Zhu Tao, Yingjie Chen and Xiangnan Hu
Affiliation:
Keywords: Vildagliptin, cost-effective, TCT.
Abstract: 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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Cite this article as:
Peng Jun, Feng Yue, Tao Zhu, Chen Yingjie and Hu Xiangnan, A Cost-Effective Method to Prepare Pure Vildagliptin, Letters in Organic Chemistry 2013; 10 (3) . https://dx.doi.org/10.2174/1570178611310030003
DOI https://dx.doi.org/10.2174/1570178611310030003 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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