Ni-Catalyzed Enantioselective C-Acylation of α-Substituted Lactams

J Am Chem Soc. 2016 Jul 27;138(29):8997-9000. doi: 10.1021/jacs.6b02120. Epub 2016 Jul 15.

Abstract

A new strategy for catalytic enantioselective C-acylation to generate α-quaternary-substituted lactams is reported. Ni-catalyzed three-component coupling of lactam enolates, benzonitriles, and aryl halides produces β-imino lactams that then afford β-keto lactams by acid hydrolysis. Use of a readily available Mandyphos-type ligand and addition of LiBr enable the construction of quaternary stereocenters on α-substituted lactams to form β-keto lactams in up to 94% ee.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Carbon / chemistry*
  • Catalysis
  • Lactams / chemistry*
  • Nickel / chemistry*
  • Stereoisomerism

Substances

  • Lactams
  • Carbon
  • Nickel