美罗列汀的合成

Synthesis of melogliptin

目的:合成二肽激肽酶IV抑制剂美罗列汀,并对工艺进行改进。方法:以(±)-2-氮杂双环[2,2,1]庚-5-烯-3-酮(2)为起始原料,通过氨基保护、还原、缩合等10步反应合成美罗列汀。结果:目标产物的结构经1H-NMR,13C-NMR和ESI-MS确证,总收率为13%。结论:该合成路线操作简单,反应条件温和,收率较高。

Objective： To synthesize melogliptin, a dipeptidyl peptidase IV inhibitor, and optimize the preparation process. Methods： The target compound was synthesized from （ ± ）-2-azabiayclo [ 2,2,1 ] hept-5-en-3- one （2） by ten steps including protection, reduction and condensation. Results： The structure of melogliptin was confirmed by ^9H-NMR, 13^C-NMR and ESI-MS. The overall yield was 13%. Conclusion： This synthetic process needs mild reaction condition, which is easy to operate with high yield.