Cross-coupling reaction of saccharide-based alkenyl boronic acids with aryl halides: the synthesis of bergenin

Chemistry. 2014 Apr 7;20(15):4414-9. doi: 10.1002/chem.201304304. Epub 2014 Mar 3.

Abstract

A convenient synthetic pathway enabling D-glucal and D-galactal pinacol boronates to be prepared in good isolated yields was achieved. Both pinacol boronates were tested in a series of cross-coupling reactions under Suzuki-Miyaura cross-coupling conditions to obtain the corresponding aryl, heteroaryl, and alkenyl derivatives in high isolated yields. This methodology was applied to the formal synthesis of the glucopyranoside moiety of papulacandin D and the first total synthesis of bergenin.

Keywords: CC coupling; glycosides; natural products; protecting groups; synthetic methods.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoglycosides / chemical synthesis
  • Aminoglycosides / chemistry
  • Benzopyrans / chemical synthesis*
  • Benzopyrans / chemistry
  • Boronic Acids / chemical synthesis
  • Boronic Acids / chemistry*
  • Echinocandins / chemical synthesis
  • Echinocandins / chemistry
  • Galactose / analogs & derivatives
  • Galactose / chemistry
  • Stereoisomerism

Substances

  • Aminoglycosides
  • Benzopyrans
  • Boronic Acids
  • Echinocandins
  • galactal
  • papulacandins
  • bergenin
  • Galactose