2-Nitro-thioglycosides: α- and β-selective generation and their potential as β-selective glycosyl donors

Org Lett. 2015 Mar 20;17(6):1421-4. doi: 10.1021/acs.orglett.5b00295. Epub 2015 Mar 5.

Abstract

Michael-type addition of thiolates to 2-nitro-D-glucal or to 2-nitro-D-galactal derivatives readily provides 2-deoxy-2-nitro-1-thioglycosides. Kinetic and thermodynamic reaction control permitted formation of either the α- or preferentially the β-anomers, respectively. Addition of achiral and chiral thiourea derivatives to the reaction mixture increased the reaction rate; the outcome is substrate-controlled. The 2-deoxy-2-nitro-1-thioglycosides are excellent glycosyl donors under arylsulfenyl chloride/silver triflate (ArSCl/AgOTf) activation, and they provide, anchimerically assisted by the nitro group, mostly β-glycosides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Combinatorial Chemistry Techniques
  • Glycosylation
  • Kinetics
  • Mesylates / chemistry
  • Molecular Structure
  • Nitro Compounds / chemical synthesis*
  • Nitro Compounds / chemistry
  • Stereoisomerism
  • Thermodynamics
  • Thioglycosides / chemical synthesis*
  • Thioglycosides / chemistry
  • Thiourea / chemistry

Substances

  • Mesylates
  • Nitro Compounds
  • Thioglycosides
  • Thiourea
  • trifluoromethanesulfonic acid