S-2-氰基吡咯烷三氟乙酸盐的合成工艺优化  

Optimization in Synthesis Process of S-2-Cyanopyrrolidine Trifluoroacetic Acid Salt

作　　者：郭丽媛[1] 董志艳[1] 吴远强 黄胜堂[1] 姚刚[1] 吴诗[1] 

机构地区：[1]湖北科技学院糖尿病心脑血管病变湖北省重点实验室,湖北咸宁437100 [2]黄石市实验高中,湖北黄石435000

出　　处：《化学与生物工程》2017年第7期31-34,共4页Chemistry & Bioengineering

基　　金：湖北科技学院糖尿病专项(ZX1016);湖北科技学院药学重点学科专项科研项目(2016-18XZY07)

摘　　要：以L-脯氨酸为原料,经二碳酸二叔丁酯保护、25%氨水溶液室温氨解、室温下脱水和脱保护得到DPP-4抑制剂重要中间体S-2-氰基吡咯烷三氟乙酸盐,4步总收率可达到50.6%。该合成方法操作简便,试剂无需浓缩,设备简单,十分适合实验室研究及小试生产。Using L-proline as a raw material,which was protected by di-tert-butyl dicarbonate,ammoniated in 25% aqueous ammonia,dehydrated and deprotected at room temperature,we synthesized an important intermediate of DPP-4 inhibitor,S-2-cyanopyrrolidine trifluoroacetic acid salt.The total yield of four steps reached 50.6%.The synthetic method is simple in operation,the reagent need not to be concentrated,and the required equipment is simple.It is very suitable for laboratory research and small test production.

关 键 词：S-2-氰基吡咯烷 DPP-4抑制剂 合成 

分 类 号：R914.2[医药卫生—药物化学]