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Author Notes:

Email: rschina@emory.edu

Dr. Schinazi is the founder and chairman of RFS Pharma, LLC. He was a Founder of Idenix and Pharmasset, Inc., now acquired by Merck and Gilead Sciences, respectively.

Subjects:

Research Funding:

National Institutes of Health, United States

This work was supported in part by NIH grants 2P30-AI-050409 and the Department of Veterans Affairs.

Keywords:

  • Science & Technology
  • Physical Sciences
  • Chemistry, Multidisciplinary
  • Chemistry
  • HEPATITIS-C VIRUS
  • ANTI-HIV ACTIVITY
  • POSSIBLE ANTIVIRAL AGENTS
  • PHOSPHORAMIDATE PROTIDE TECHNOLOGY
  • REPLICATION IN-VITRO
  • ACYCLOVIR DIPHOSPHATE DIMYRISTOYLGLYCEROL
  • PRELIMINARY BIOLOGICAL EVALUATION
  • ARYL PHOSPHOTRIESTER DERIVATIVES
  • LIPOPHILIC NUCLEOTIDE PRODRUGS
  • TOXIC LIPONUCLEOTIDE ANALOGS

Synthesis of Nucleoside Phosphate and Phosphonate Prodrugs

Tools:

Journal Title:

Chemical Reviews

Volume:

Volume 114, Number 18

Publisher:

, Pages 9154-9218

Type of Work:

Article | Final Publisher PDF

Abstract:

The article reviews the most important mono-, di-, and triphosphate and phosphonate prodrug approaches applied to nucleoside analogs from a chemical point of view, detailing the strengths and limitations of each approach. The article focuses on the various synthetic pathways discussing the chemical variation of the biolabile phosph(on)ate masking groups, the reliability of using P(III) and/or P(V) chemistry for phosphate and phosphonate prodrug synthesis, and the influence of the masking group(s) introduction conditions on the overall outcome for each method.

Copyright information:

© 2014 American Chemical Society.ACS AuthorChoice - This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.

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