Synthesis of 2',3'-dideoxyisoguanosine from guanosine

Arch Pharm Res. 1999 Dec;22(6):619-23. doi: 10.1007/BF02975335.

Abstract

2,3'-Dideoxyisoguanosine was synthesized from guanosine via intermediate 6-[(4-methylphenyl)thio]-2-oxo-9-(2',3',5'-tri-O-acetyl-beta-D-ribofuran osyl)-2,3-dihydropurine (4). The 2-oxo, 6-amino and 5'-hydroxy triprotected isoguanosine derivative was utilized to reduce high polarity and promote poor solubility of intermediates. The protecting groups for oxo and 6-amino were easily removed in reduction of olefin in ribose without additional reaction steps. 2',3'-Vicinal diol in ribose sugar moiety was transformed to olefin with Bu3SnH by radical reaction via bisxanthate. Removing 5'-O-TBDMS protecting group gave final product, 2',3'-dideoxyisoguanosine (12) in a 10% overall yield.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry
  • Antiviral Agents / chemical synthesis
  • Dideoxynucleosides / chemical synthesis*
  • Guanosine / chemistry*
  • Ribose / chemistry
  • Solubility

Substances

  • Alkenes
  • Antiviral Agents
  • Dideoxynucleosides
  • Guanosine
  • Ribose
  • 2',3'-dideoxyguanosine