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Synfacts 2010(7): 0742-0742
DOI: 10.1055/s-0029-1220018
DOI: 10.1055/s-0029-1220018
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag
Stuttgart ˙ New York
Synthesis of Vaniprevir (MK-7009)
et al. J. A. McCauley*
Merck Research Laboratories, West Point, USA
Further Information
Publication History
Publication Date:
22 June 2010 (online)
Significance
Vaniprevir (MK-7009) is a clinical candidate for the treatment of hepatitis C. It is an HCV NS3/4a protease inhibitor with good plasma and liver exposure in multiple species. The key step in the synthesis is a stereoselective ring-closing metathesis of dilute solutions (3 mM) of the diene G using the Zhan catalyst H.