Synthesis of [14C]boceprevir, [13C 3]boceprevir, and [D9]boceprevir, a hepatitis C virus protease inhibitor
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%. Copyright 2012 John Wiley & Sons, Ltd. Boceprevir is an 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 4 steps with an overall yield of 69%.
Ren, Sumei,Royster, Pernilla,Lavey, Carolee,Hesk, David,McNamara, Paul,Koharski, David,Truong, Van,Borges, Scott
experimental part
p. 108 - 114
(2012/07/17)
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