Enantioselective Friedel–Crafts alkylation reaction of indoles with α,β-unsaturated acyl phosphonates catalyzed by chiral phosphoric acid

Abstract

A variety of indoles underwent enantioselective Friedel-Crafts alkylation with alpha,beta-unsaturated acyl phosphonates in the presence of 10 mol% chiral BINOL-based phosphoric acid and subsequent treatment with methanol and DBU to give methyl 3-(indol-3-yl)propanoates in good yields and with high enantioselectivities.