2型糖尿病治疗药物托格列净的合成路线图解  

Graphical synthetic routes of Tofogliflozin for type 2 diabetes mellitus treatment

作　　者：胡家栋 文雯 宋慧颖 李博[1] 姚宇 HU Jiadong;WEN Wen;SONG Huiying;Li Bo;YAO Yu(School of Medicinal and Chemical Engineering,Yangling Vocational&Technical College,Yangling 712100,China;College of Chemistry&Pharmacy,Northwest A&F University,Yangling 712100,China)

机构地区：[1]杨凌职业技术学院药物与化工学院,陕西杨凌712100 [2]西北农林科技大学化学与药学院,陕西杨凌712100

出　　处：《广东药科大学学报》2021年第4期145-150,共6页Journal of Guangdong Pharmaceutical University

基　　金：陕西高校青年创新团队(陕教[2020]137号);陕西省自然科学基础研究计划(2020JQ-993);杨凌职业技术学院自然科学研究基金资助项目(ZK20-72)。

摘　　要：托格列净是一种高选择性的钠-葡萄糖协同转运蛋白2抑制剂,属于非胰岛素依赖型降糖药物,于2014年在日本上市用于治疗2型糖尿病。本文从亲核加成-直接环合法和[4+2]环加成法2个构建螺缩酮结构的角度总结了目前报道的5条托格列净合成路线的特点,以期为后期的市场化进程提供参考。Tofogliflozin is a highly selective sodium glucose co-transporter 2 inhibitor,which is a non-insulin dependent hypoglycemic drug.It was marketed in Japan in 2014 for the treatment of type 2 diabetes mellitus.In this paper,the characteristics of five synthetic routes of Tofogliflozin were summarized from the perspectives of nucleophilic addition direct cycloaddition and[4+2]cycloaddition to construct spiroketalstructures.so as to provide a reference for the later marketization process.

关 键 词：托格列净 钠-葡萄糖协同转运蛋白2抑制剂 2型糖尿病 非胰岛素依赖型 

分 类 号：R914.5[医药卫生—药物化学]