Synthesis of [14C] boceprevir,[13C3] boceprevir, and [D9] boceprevir, a hepatitis C virus protease inhibitor

…, P McNamara, D Koharski, V Truong…

Index: Ren, Sumei; Royster, Pernilla; Lavey, Carolee; Hesk, David; McNamara, Paul; Koharski, David; Truong, Van; Borges, Scott Journal of Labelled Compounds and Radiopharmaceuticals, 2012 , vol. 55, # 3 p. 108 - 114

Full Text: HTML

Citation Number: 1

Abstract

Boceprevir is a hepatitis C virus (HCV) NS3 protease inhibitor for HCV treatment.[14C] Boceprevir (SCH 503034, trade name Victrelis) was synthesized from K14CN in 11 steps with an overall yield of 16.4%.[13C3] Boceprevir was synthesized in 16 steps with a 2.5% overall yield. The carbon-13 in the molecule was distributed along the peptide chain.[D9] Boceprevir was synthesized from [D9]-t-butylamine in four steps with an overall yield of 69 ...