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.
LIN DaiZongQIAN WangKeHILGENFELD RolfJIANG HuaLiangCHEN KaiXianLIU Hong
<正>Isocoumarins are key core structural subunits that occur in a wide variety of biologically active natural p...
Guannan Liu,~a Yu Zhou,~a Deju Ye,~a Dengyou Zhang,~a Xiao Ding,~a Hualiang Jiang,~a Hong Liu~(a,*) a Drug Discovery and Design Centre,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological Sciences,Chinese Academy of Science 555 Zuchongzhi Road,Shanghai 201203,China