Modular Synthesis of Constrained Ethyl (cEt) Purine and Pyrimidine Nucleosides

J Org Chem. 2015 May 15;80(10):5337-43. doi: 10.1021/acs.joc.5b00607. Epub 2015 Apr 28.

Abstract

A modular and scalable approach to pyrimidine- and purine-containing constrained ethyl (cEt) nucleosides is demonstrated. Minimizing stereochemical adjustments and protecting group manipulations, diacetone glucose is converted to two representative cEt nucleosides via a functionalized, common intermediate. The retrosynthetic approach to this complex class of drug precursors offers clear benefits over existing routes based on step count and efficiency.

MeSH terms

  • Molecular Structure
  • Nucleosides / chemical synthesis*
  • Nucleosides / chemistry
  • Prodrugs / chemical synthesis*
  • Prodrugs / chemistry
  • Purine Nucleosides / chemical synthesis*
  • Purine Nucleosides / chemistry
  • Pyrimidine Nucleosides / chemical synthesis*
  • Pyrimidine Nucleosides / chemistry

Substances

  • Nucleosides
  • Prodrugs
  • Purine Nucleosides
  • Pyrimidine Nucleosides