Improved synthesis of rupintrivir  

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

机构地区：[1]State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China [2]School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China [3]Institute of Biochemistry, Center for Structural and Cell Biology in Medicine, University of Luebeck, 23538 Luebeck, Germany

出　　处：《Science China Chemistry》2012年第6期1101-1107,共7页中国科学（化学英文版）

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)

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.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 con- structed 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.

关 键 词：rupintrivir AG7088 SYNTHESIS 

分 类 号：TQ560.6[化学工程—炸药化工] TQ464.71