Improved synthesis of rupintrivir

作     者：LIN DaiZong QIAN WangKe HILGENFELD Rolf JIANG HuaLiang CHEN KaiXian LIU Hong 

作者机构：State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China Institute of Biochemistry Center for Structural and Cell Biology in Medicine University of Luebeck 23538 Luebeck Germany 

出 版 物：《Science China Chemistry》 (中国科学（化学英文版）)

年 卷 期：2012年第55卷第6期

页      面：1101-1107页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 100705[医学-微生物与生化药学] 082604[工学-军事化学与烟火技术] 08[工学] 0826[工学-兵器科学与技术] 10[医学] 

基　　金：financial support from the National Natural Science Foundation of China (20872153, 21021063, 20720102040 and81025017) the National Basic Research Program of China grant(2009CB918502) the Chinese Academy of Sciences (XDA01040305) the SILVER project of the European Commission (contract HEALTH-F3-2010-260644) supported by a Chinese Academy of Sciences Visiting Professorship for Senior International Scientists (2010T1S6) 

主　　题：rupintrivir AG7088 synthesis 

摘      要：An improved synthesis of rupintrivir (AG7088) was accomplished using three amino acids (L-glutamic acid, D-4-fluorophenylalanine, and L-valine) as the building blocks. The key fragment ketomethylene dipeptide isostere was constructed with the valine derivative and phenylpropionic acid derivative, followed by coupling with a lactam derivative and an isoxazole acid chloride to provide AG7088 totally in eight steps.