Synthesis of substituted septanosyl-1,2,3-triazoles

Carbohydr Res. 2007 Jul 23;342(10):1366-72. doi: 10.1016/j.carres.2007.03.026. Epub 2007 Apr 2.

Abstract

A carbohydrate-based oxepine, derived from 2-deoxy-D-arabino-hexopyranose, was used to prepare a family of septanosyl-1,2,3-triazoles in four steps. DMDO mediated epoxidation of the oxepine followed by trapping of the intermediate 1,2-anhydroseptanose by sodium azide gave the beta-substituted glycosyl azide. The septanosyl azide was then reacted with a number of alkynes under thermal Huisgen or copper(I) mediated reaction conditions. Hydrogenolysis of benzyl protecting groups gave substituted septanosyl-1,2,3-triazoles. The new septanose-based structures were then evaluated as potential glycosidase inhibitors.

Publication types

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

MeSH terms

  • Carbohydrate Conformation
  • Carbohydrate Sequence
  • Glycoside Hydrolases / analysis
  • Glycoside Hydrolases / antagonists & inhibitors*
  • Glycoside Hydrolases / classification
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Nitrogen / chemistry
  • Oxepins / chemistry
  • Spectrophotometry, Ultraviolet
  • Temperature
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

  • Oxepins
  • Triazoles
  • Glycoside Hydrolases
  • Nitrogen