An enantioselective synthesis of voriconazole

J Org Chem. 2013 Nov 15;78(22):11396-403. doi: 10.1021/jo4019528. Epub 2013 Oct 25.

Abstract

A new seven-step sequence to access voriconazole, a clinically used antifungal agent, was developed. The initial catalytic asymmetric cyanosilylation is the key to constructing the consecutive tetra- and trisubstituted stereogenic centers. The fluoropyrimidine unit frequently triggered unexpected side reactions, but careful amendment of the reaction sequence allowed for the concise enantioselective synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Molecular Structure
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Stereoisomerism
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Voriconazole

Substances

  • Pyrimidines
  • Triazoles
  • Voriconazole