Development of a Kilogram-Scale Synthesis of a Novel Anti-HCV Agent, CH4930808

摘要

Herein, we report the kilogram-scale synthesis of CH4930808 (1), a novel anti-hepatitis C virus agent. While pursuing improved productivity using many through-process strategies, we conducted scrupulous impurity control. Finally, we successfully developed a practical and scalable process for the synthesis of (1-1.5Na center dot 2.5H(2)O), by which we prepared 3.28 kg of the active pharmaceutical ingredient for clinical studies.