Enantioselective Friedel–Crafts alkylation reaction of indoles with α,β-unsaturated acyl phosphonates catalyzed by chiral phosphoric acid†
Prabhakar Bachu,Takahiko Akiyama
Chemical Communications Pub Date : 03/16/2010 00:00:00 , DOI:10.1039/C000862A
Abstract

A variety of indoles underwent enantioselective Friedel–Crafts alkylation with α,β-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.

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