2. Academic Validation
  3. Synthesis and anti-HCV activity of β-d-2'-deoxy-2'-α-chloro-2'-β-fluoro and β-d-2'-deoxy-2'-α-bromo-2'-β-fluoro nucleosides and their phosphoramidate prodrugs

Synthesis and anti-HCV activity of β-d-2'-deoxy-2'-α-chloro-2'-β-fluoro and β-d-2'-deoxy-2'-α-bromo-2'-β-fluoro nucleosides and their phosphoramidate prodrugs

  • Bioorg Med Chem. 2019 Feb 15;27(4):664-676. doi: 10.1016/j.bmc.2019.01.005.
Reuben Ovadia 1,  Ahmed Khalil 1,  Hao Li 1,  Coralie De Schutter 1,  Seema Mengshetti 1,  Shaoman Zhou 1,  Leda Bassit 1,  Steven J Coats 1,  Franck Amblard 1,  Raymond F Schinazi 2
Affiliations

Affiliations

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
  • 2 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. Electronic address: rschina@emory.edu.
PMID: 30655167 DOI: 10.1016/j.bmc.2019.01.005
Abstract

We report herein the synthesis and evaluation of a series of β-d-2'-deoxy-2'-α-chloro-2'-β-fluoro and β-d-2'-deoxy-2'-α-bromo-2'-β-fluoro nucleosides along with their corresponding phosphoramidate prodrugs. Key intermediates, lactols 11 and 12, were obtained by a diastereoselective fluorination of protected 2-deoxy-2-chloro/bromo-ribonolactones 7 and 8. All synthesized nucleosides and prodrugs were evaluated with a hepatitis C virus (HCV) subgenomic replicon system.

Keywords

Antivirals; Fluorination; Nucleosides; Prodrugs.

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