InBr3-catalyzed glycosidation of glycals with arylamines: an alternative approach to access 4-aminocyclopent-2-enones

J Org Chem. 2011 Apr 15;76(8):2820-7. doi: 10.1021/jo200243d. Epub 2011 Mar 17.

Abstract

To turn side products into major products, a novel strategy to access biologically active 4-aminocyclopent-2-enones was developed. These compounds were originally identified as side products but became major products when 3,5-dimethylpyran-3,4-diol 7a was used as the substrate and 30% InBr(3) as the catalyst. Aryl- or heteroarylamines as well as variously substituted glycals can be used in this reaction, and the corresponding 4-aminocyclopent-2-enones were obtained in moderate to good yields. These compounds can be further used to prepare 4-aminocarbocyclic nucleosides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry
  • Antiviral Agents / chemical synthesis*
  • Catalysis
  • Cyclopentanes / chemical synthesis*
  • Glycosides / chemistry
  • Indium / chemistry*
  • Molecular Structure
  • Nucleosides / chemical synthesis
  • Prostaglandins / chemistry
  • Stereoisomerism

Substances

  • Amines
  • Antiviral Agents
  • Cyclopentanes
  • Glycosides
  • Nucleosides
  • Prostaglandins
  • indium bromide
  • Indium
  • cyclopentanone