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Synfacts 2010(2): 0141-0141  
DOI: 10.1055/s-0029-1219035
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

HCV NS5B Inhibitor PSI-6130

Contributor(s): Philip Kocienski
P. Wang, B.-K. Chun, S. Rachakonda, J. Du, N. Khan, J. Shi, W. Stec, D. Cleary, B. S. Ross*, M. J. Sofia
Pharmasset, Inc., Princeton, USA and Polish Academy of Sciences, Lodz, Poland
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Publication History

Publication Date:
21 January 2010 (online)

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Significance

PSi-6130 is a ribonucleoside analogue that is currently in phase IIb clinical trials for the treatment of hepatitis C. It is the first direct acting antiviral to display potent activity against both genotype 2 and 3 virus. A major challenge in the synthesis was the efficient installation of the C-2′ fluorinated quaternary center. This was accomplished via regioselective nucleophilic opening of the cyclic sulfate D with Me4NF.