Direct catalytic asymmetric alkynylation of ketoimines

Org Lett. 2013 Feb 1;15(3):698-701. doi: 10.1021/ol3035609. Epub 2013 Jan 18.

Abstract

An efficient protocol for direct catalytic alkynylation of ketoimines is described. The simultaneous activation of a soft Lewis basic terminal alkyne and a ketoimine bearing a thiophosphinoyl group by soft Lewis acid Cu(I) is crucial for high conversion. The reaction can be rendered asymmetric with a chiral bisphosphine ligand (S,S)-Ph-BPE.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemical synthesis
  • Alkynes / chemistry*
  • Catalysis
  • Combinatorial Chemistry Techniques
  • Imines / chemistry*
  • Lewis Acids / chemistry
  • Stereoisomerism

Substances

  • Alkynes
  • Imines
  • Lewis Acids