Synfacts 2011(8): 0810-0810  
DOI: 10.1055/s-0030-1260674
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of PSI-352938

Contributor(s): Philip Kocienski
P. G. Reddy, B.-K. Chun, H.-R. Zhang, S. Rachakonda, B. S. Ross*, M. J. Sofia
Pharmasset, Inc., Princeton, USA
Further Information

Publication History

Publication Date:
20 July 2011 (online)

Significance

PSI-352938 is an orally active, ­nucleotide prodrug that inhibits HCV NS5B polymerase. It is currently in clinical trials for the treatment of hepatitis C. Noteworthy features include broad genotype coverage and a good resistance profile. The synthesis depicted delivered multikilogram quantities of API without recourse to chromatography.