An in Situ Approach to Nickel-Catalyzed Cycloaddition of Alkynes and 3-Azetidinones

J Org Chem. 2015 Oct 16;80(20):9951-8. doi: 10.1021/acs.joc.5b01458. Epub 2015 Oct 6.

Abstract

An efficient and convenient procedure that generates the active Ni(0) catalyst in situ from cheap, air stable Ni(II) precursors is developed for the [4 + 2]-cycloaddition of alkynes and 3-azetidinones. The reaction affords useful 3-dehydropiperidinones in comparable yields to the reported Ni(0) procedure. Additionally, the cycloaddition with 3-oxetanone afforded the 3-dehydropyranone product. Chiral 2-substituted azetidinones were also tolerated to form substituted dehydropiperidinones in high yield and enantiomeric excess.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alkynes / chemistry*
  • Azetidines / chemistry*
  • Catalysis
  • Cyclization
  • Molecular Structure
  • Nickel / chemistry*
  • Piperidones / chemical synthesis*
  • Piperidones / chemistry

Substances

  • Alkynes
  • Azetidines
  • Piperidones
  • Nickel