Formal Glycosylation of Quinones with exo-Glycals Enabled by Iron-Mediated Oxidative Radical-Polar Crossover

J Org Chem. 2022 Oct 7;87(19):13178-13194. doi: 10.1021/acs.joc.2c01635. Epub 2022 Sep 12.

Abstract

The intermolecular C-O coupling reaction of 1,4-quinones with exo-glycals under iron hydride hydrogen atom transfer (HAT) conditions is described. This method provides a direct and regioselective access to a wide range of phenolic O-ketosides related to biologically relevant natural products in diastereomeric ratios up to >98:2 in the furanose and pyranose series. No trace of the corresponding C-glycosylated products that might have resulted from the radical alkylation of 1,4-quinones was observed. The results of mechanistic experiments suggest that the key C-O bond-forming event proceeds through an oxidative radical-polar crossover process involving a single-electron transfer between the HAT-generated glycosyl radical and the electron-acceptor quinone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Products*
  • Glycosylation
  • Hydrogen
  • Iron*
  • Oxidative Stress
  • Quinones

Substances

  • Biological Products
  • Quinones
  • Hydrogen
  • Iron