Stereoselective C-glycosylation reactions with arylzinc reagents

Org Lett. 2012 Mar 16;14(6):1480-3. doi: 10.1021/ol300220p. Epub 2012 Mar 2.

Abstract

A general, transition-metal-free, highly stereoselective cross-coupling reaction between glycosyl bromides and various arylzinc reagents leading to β-arylated glycosides is reported. The stereoselectivity of the reaction is explained by invoking anchimeric assistance via a bicyclic intermediate. Stereochemical probes confirm the participation of the 2-pivaloyloxy group. Finally, this new method was applied to a short and efficient stereoselective synthesis of Dapagliflozin and Canagliflozin.

MeSH terms

  • Benzhydryl Compounds
  • Glucosides / chemical synthesis*
  • Glucosides / chemistry
  • Indicators and Reagents / chemistry
  • Molecular Structure
  • Stereoisomerism

Substances

  • Benzhydryl Compounds
  • Glucosides
  • Indicators and Reagents
  • dapagliflozin