Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 2, Pages 64-69Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml9000276
Keywords
Hepatitis C virus NS3 serine protease inhibitor; alpha-ketoamide; narlaprevir; SCH 900518
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Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials. Detailed investigations toward a second generation protease inhibitor culminated in the discovery of narlaprevir (SCH 900518), 37, with improved potency (similar to 10-fold over 1), pharmacokinetic profile and physicochemical characteristics, currently in phase II human trials. Exploration of synthetic sequence for preparation of 37 resulted in a route that required no silica gel purification for the entire synthesis.
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