A Cost-Effective Method to Prepare Pure Vildagliptin

被引：4
作者：
Peng, Jun [1 ]
Feng, Yue [1 ]
Tao, Zhu [1 ]
Chen, Yingjie [1 ]
Hu, Xiangnan [1 ]
机构：
[1] Chongqing Med Univ, Dept Pharm, Chongqing 400016, Peoples R China
来源：
LETTERS IN ORGANIC CHEMISTRY | 2013年 / 10卷 / 03期
关键词：
Vildagliptin; cost-effective; TCT; DIPEPTIDYL PEPTIDASE-IV; GLUCAGON-LIKE PEPTIDE-1; INHIBITOR; POTENT;
D O I：
10.2174/1570178611310030003
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
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%.
引用
收藏
页码：159 / 163
页数：5
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