Enantioselective Friedel-Crafts alkylation of indoles with trifluoroethylidene malonates by copper-bis(oxazoline) complexes: construction of trifluoromethyl-substituted stereogenic tertiary carbon center

J Org Chem. 2011 Apr 1;76(7):2282-5. doi: 10.1021/jo1024333. Epub 2011 Mar 4.

Abstract

An enantioselective alkylation of indoles with trifluoroethylidene malonates catalyzed by copper(II)-bis (oxazoline) complexes has been developed. The expected adducts with a stereogenic tertiary carbon center bearing a trifluoromethyl group were obtained in excellent yields (up to 99%) and ee values (up to 96% ee). The synthetic utility of this asymmetric catalytic reaction was demonstrated by the preparation of β-CF(3)-tryptophan and 4-CF(3)-β-carboline in high ee.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Carbon / chemistry*
  • Catalysis
  • Copper / chemistry*
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry*
  • Indoles / chemistry*
  • Malonates / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Hydrocarbons, Fluorinated
  • Indoles
  • Malonates
  • Carbon
  • Copper