Synthesis of [ 14 C]boceprevir, [ 13 C 3 ]boceprevir, and [D 9 ]boceprevir, a hepatitis C virus protease inhibitor | Zendy

Ren Sumei | Zendy; Royster Pernilla | Zendy; Lavey Carolee | Zendy; Hesk David | Zendy; McNamara Paul | Zendy; Koharski David | Zendy; Truong Van | Zendy; Borges Scott | Zendy

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Synthesis of [ 14 C]boceprevir, [ 13 C 3 ]boceprevir, and [D 9 ]boceprevir, a hepatitis C virus protease inhibitor

Author(s) -

Ren Sumei,

Royster Pernilla,

Lavey Carolee,

Hesk David,

McNamara Paul,

Koharski David,

Truong Van,

Borges Scott

Publication year - 2012

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/jlcr.1960

Subject(s) - boceprevir , virology , chemistry , hepatitis c virus , protease inhibitor (pharmacology) , protease , ns3 , virus , medicine , biochemistry , ribavirin , enzyme , viral load , antiretroviral therapy

Boceprevir is a hepatitis C virus (HCV) NS3 protease inhibitor for HCV treatment. [ 14 C]Boceprevir (SCH 503034, trade name Victrelis) was synthesized from K 14 CN in 11 steps with an overall yield of 16.4%. [ 13 C 3 ]Boceprevir was synthesized in 16 steps with a 2.5% overall yield. The carbon‐13 in the molecule was distributed along the peptide chain. [D 9 ]Boceprevir was synthesized from [D 9 ]‐ t ‐butylamine in four steps with an overall yield of 69%. Copyright © 2012 John Wiley & Sons, Ltd.

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