Improved synthesis of rupintrivir

…, WK Qian, R Hilgenfeld, HL Jiang, KX Chen…

Index: Lin, Daizong; Qian, Wangke; Hilgenfeld, Rolf; Jiang, Hualiang; Chen, Kaixian; Liu, Hong Science China Chemistry, 2012 , vol. 55, # 6 p. 1101 - 1107

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Abstract

Abstract 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.