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...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.展开更多
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)+2 种基金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)
文摘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.