Synthesis of L-3'-hydroxymethylribonucleosides

Nucleosides Nucleotides Nucleic Acids. 2000 Jan-Feb;19(1-2):219-36. doi: 10.1080/15257770008033005.

Abstract

The target compounds were synthesized via the key intermediate carbohydrate 8, which was synthesized by first selectively protecting the 1'- and 2'-hydroxyl groups followed by selective tosylation of the 5'-hydroxyl group to obtain compound 3. The tosyl moiety was then replaced by a benzyl either to obtain 4. Compound 4 underwent Dess-Martin oxidation to afford the ketone 5. Compound 5 was subjected to Wittig olefination to afford the alkene 6 followed by regioselective hydroboration to obtain 7. Compound 7 was fully acetylated using acetic acid, acetic anhydride and sulfuric acid to obtain the key intermediate 8.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetylation
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • HIV-1 / drug effects
  • Hepatitis B virus / drug effects
  • Humans
  • In Vitro Techniques
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / virology
  • Magnetic Resonance Spectroscopy
  • Ribonucleosides / chemical synthesis*
  • Ribonucleosides / chemistry
  • Ribonucleosides / pharmacology
  • Stereoisomerism

Substances

  • Anti-HIV Agents
  • Antiviral Agents
  • Ribonucleosides