琥珀酸曲格列汀的合成  

Synthesis of trelagliptin succinate

作　　者：江洁滢 游莉[1] 邓思思[1] 邓俊丰[1] 刘瑜[1] 张晓[1] 

机构地区：[1]四川抗菌素工业研究所,成都610052

出　　处：《中国新药杂志》2015年第16期1876-1878,1910,共4页Chinese Journal of New Drugs

摘　　要：目的:合成二肽基肽酶IV抑制剂曲格列汀,并对合成路线进行改进。方法:以2-溴-5-氟甲苯(2)为原料,经偶联上氰基、自由基反应、取代等制得曲格列汀三氟乙酸盐,碱解后成盐得到曲格列汀琥珀酸盐。结果:目标产物经1H-NMR,ESI-MS确认,总产率19.1%。结论:该合成路线操作简单,反应条件温和,收率较高。Objective： To synthesis trelagliptin, a dipeptidyl peptidasel IV inhibitor, and optimize the preparation process. Methods： The target compound was synthesized 1 -bromo-4-fluoro-2-methyl-benzene （ 2 ） by five steps including cross-coupling, radical reaction and substitution. Results： The structure of trelagliptin was confirmed by 1H-NMR and ESI-MS. The overall yield was 19.1%. Conclusion： This synthetic process needs mild reaction condition, which is easy to prepare with high yield.

关 键 词：曲格列汀 二肽基肽酶IV抑制剂 合成 

分 类 号：R914.5[医药卫生—药物化学]