Enantioselective Friedel-Crafts Alkylation Reactions of 3-Substituted Indoles with Electron-Deficient Alkenes

J Org Chem. 2016 Apr 1;81(7):3023-30. doi: 10.1021/acs.joc.6b00123. Epub 2016 Mar 15.

Abstract

Highly enantioselective Friedel-Crafts C2-alkylation reactions of 3-substituted indoles with α,β-unsaturated esters and nitroalkenes were developed using chiral Lewis acids as catalysts, which afforded chiral indole derivatives bearing C2-benzylic stereogenic centers in good to excellent yields (up to 99%) and enantioselectivities (up to 96% ee).

Publication types

  • Research Support, Non-U.S. Gov't