Development of the Enabling Route for a Novel HCV NS3/4A Inhibitor, Furaprevir

Furaprevir demonstrated adequate safety and effectiveness in clinical phases I and II, which was identified as a potent Hepatitis C virus (HCV) NS3/4A protease inhibitor. Research on the synthesis process of Furaprevir is insufficient, so a reliable manufacturing procedure is required to support subsequent clinical trials. There were two challenging steps in the synthesis process, which involved an amide-bond formation and a ring-closing metathesis (RCM) reaction to form the product active pharmaceutical ingredient (API). The optimized process conditions were successfully used to produce 25 kg per batch of Furaprevir, which was sufficient to support the subsequent clinical development and onward.