Access to 3-O-Functionalized N-Acetylneuraminic Acid Scaffolds

J Org Chem. 2015 Aug 7;80(15):7746-51. doi: 10.1021/acs.joc.5b00992. Epub 2015 Jul 14.

Abstract

Direct access to 3-O-functionalized 2-α-N-acetylneuraminides and their corresponding 2,3-dehydro-2-deoxy-N-acetylneuraminic acid derivatives is described. Initially, a stereoselective ring-opening of the key intermediate N-acetylneuraminic acid (Neu5Ac) 2,3-β-epoxide with an alcohol provided the 3-hydroxy α-glycoside. O-Alkylation of the C3 hydroxyl group generated novel 3-O-functionalized Neu5Ac derivatives that provided the corresponding unsaturated derivatives upon elimination.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Glycosides / chemistry*
  • Magnetic Resonance Spectroscopy
  • N-Acetylneuraminic Acid / analogs & derivatives*
  • N-Acetylneuraminic Acid / chemical synthesis
  • N-Acetylneuraminic Acid / chemistry
  • Sialic Acids / chemical synthesis*
  • Sialic Acids / chemistry
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Glycosides
  • Sialic Acids
  • 2-deoxy-2,3-dehydro-N-acetylneuraminic acid
  • N-Acetylneuraminic Acid