High-pressure accelerated asymmetric organocatalytic Friedel-Crafts alkylation of indoles with enones: application to quaternary stereogenic centers construction

Org Lett. 2012 Mar 16;14(6):1540-3. doi: 10.1021/ol300274u. Epub 2012 Mar 7.

Abstract

An organocatalytic Friedel-Crafts alkylation of indoles with α,β-unsaturated ketones was found to be efficiently accelerated under high-pressure conditions with a low loading of chiral primary amine salts with good yield and enantioselectivity up to 90%. This approach also allows, for the first time, selected indole derivatives containing quaternary stereogenic centers to be obtained from prochiral β,β-disubstituted enones with an enantioselectivity up to 80%.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Amines / chemistry*
  • Catalysis
  • Indoles / chemical synthesis*
  • Indoles / chemistry*
  • Ketones / chemical synthesis*
  • Ketones / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Amines
  • Indoles
  • Ketones