C2-hydroxyglycosylation with glycal donors. Probing the mechanism of sulfonium-mediated oxygen transfer to glycal enol ethers

J Am Chem Soc. 2002 Jun 26;124(25):7343-52. doi: 10.1021/ja025639c.

Abstract

The C2-hydroxyglycosylation reaction employing the reagent combination of a diaryl sulfoxide and triflic anhydride offers a novel method for glycal assembly whereby a hydroxyl functionality is stereoselectively installed at the C2-position of a glycal donor with concomitant glycosylation of a nucleophilic acceptor. Mechanistic investigations into this reaction revealed a novel process for sulfonium-mediated oxidation of glycal enol ethers in which the sulfoxide oxygen atom is stereoselectively transferred to the C2-position of the glycal. (18)O-labeling studies revealed that the S-to-C2 oxygen-transfer process involves initial formation of a C1[bond]O linkage followed by O-migration to C2, leading to the generation of an intermediate glycosyl 1,2-anhydropyranoside that serves as an in situ glycosylating agent. These findings are consistent with the initial formation of a C2-sulfonium[bond]C1-oxosulfonium pyranosyl species upon activation of the glycal donor with Aryl(2)SO x Tf(2)O.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Anhydrides / chemistry
  • Ethers / chemistry
  • Glycosylation
  • Oligosaccharides / chemical synthesis*
  • Oligosaccharides / chemistry*
  • Oxygen / chemistry*
  • Stereoisomerism
  • Sulfoxides / chemistry*

Substances

  • Anhydrides
  • Ethers
  • Oligosaccharides
  • Sulfoxides
  • Oxygen