Concepedia

Synthesis of Grazoprevir, a Potent NS3/4a Protease Inhibitor for the Treatment of Hepatitis C Virus

Feng Xu, Jungchul Kim, Jacob H. Waldman, Tao Wang, Paul N. Devine

Organic Letters · 2018 · 25 citations · 10 references

DOI

Concepts

Abstract

An efficient synthesis of grazoprevir is reported. Starting from four readily available building blocks, grazoprevir is prepared in 51% overall yield and >99.9% purity for pharmaceutical use.

References

10

Isolation of a cDNA cLone Derived from a Blood-Borne Non-A, Non-B Viral Hepatitis Genome

Qui‐Lim Choo, George Kuo, Amy J. Weiner et al. · Science · 1989 · 6.9K citations

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Single-Electron Transmetalation: An Enabling Technology for Secondary Alkylboron Cross-Coupling

David N. Primer, İdris Karakaya, John C. Tellis et al. · Journal of the American Chemical Society · 2015 · 320 citations

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Efficacy and safety of 12 weeks versus 18 weeks of treatment with grazoprevir (MK-5172) and elbasvir (MK-8742) with or without ribavirin for hepatitis C virus genotype 1 infection in previously untreated patients with cirrhosis and patients with previous null response with or without cirrhosis (C-WORTHY): a randomised, open-label phase 2 trial

Eric Lawitz, Edward Gane, Brian L. Pearlman et al. · The Lancet · 2014 · 300 citations

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Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor

Steven J. Harper, John A. McCauley, Michael T. Rudd et al. · ACS Medicinal Chemistry Letters · 2012 · 201 citations · Full text

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One-Step RhCl<sub>3</sub>-Catalyzed Deprotection of Acyclic <i>N</i>-Allyl Amides

Michael J. Zacuto, Feng Xu · The Journal of Organic Chemistry · 2007 · 69 citations

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