Enantioselective [4 + 2] cycloaddition of cyclic N-sulfimines and acyclic enones or ynones: a concise route to sulfamidate-fused 2,6-disubstituted piperidin-4-ones

Org Lett. 2013 Dec 6;15(23):6090-3. doi: 10.1021/ol402977w. Epub 2013 Nov 12.

Abstract

A concise route to valuable sulfamate-fused 2,6-disubstituted piperidin-4-ones or 2,3-dihydropyridin-4(1H)-ones in good yield with high diastereo- and enantioselectivity is presented. The combination of chiral primary amine and o-fluorobenzoic acid efficiently promoted an asymmetric [4 + 2] cycloaddition reaction of N-sulfonylimines and enones or ynones. The cycloaddition reaction between cyclic N-sulfonylimines and ynones is first reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry
  • Catalysis
  • Cyclization
  • Cycloaddition Reaction
  • Imines / chemistry
  • Ketones / chemistry
  • Molecular Structure
  • Piperidones / chemical synthesis*
  • Piperidones / chemistry
  • Stereoisomerism
  • Sulfones / chemical synthesis*
  • Sulfones / chemistry

Substances

  • Amines
  • Imines
  • Ketones
  • Piperidones
  • Sulfones