Scope and limitations of 2-deoxy- and 2,6-dideoxyglycosyl bromides as donors for the synthesis of β-2-deoxy- and β-2,6-dideoxyglycosides

Org Lett. 2014 May 16;16(10):2776-9. doi: 10.1021/ol501101f. Epub 2014 May 1.

Abstract

It is shown that 2-deoxy- and 2,6-dideoxyglycosyl bromides can be prepared in high yield (72-94%) and engaged in glycosylation reactions with β:α selectivities ≥6:1. Yields of product are 44-90%. Fully armed 2-deoxyglycoside donors are viable, while 2,6-dideoxyglycosides require one electron-withdrawing substituent for high efficiency and β-selectivity. Equatorial C-3 ester protecting groups decrease β-selectivity, and donors bearing an axial C-3 substituent are not suitable. The method is compatible with azide-containing donors and acid-sensitive functional groups.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Azides / chemistry
  • Combinatorial Chemistry Techniques
  • Electrons
  • Glycosides / chemical synthesis*
  • Glycosides / chemistry
  • Glycosylation
  • Hydrocarbons, Brominated / chemical synthesis*
  • Hydrocarbons, Brominated / chemistry
  • Molecular Structure
  • Stereoisomerism

Substances

  • Azides
  • Glycosides
  • Hydrocarbons, Brominated