Abstract

A highly enantioselective aza-Friedel-Crafts alkylation of indoles with cyclic aryl α-ketimino esters catalyzed by a chiral phosphoric acid has been developed, the corresponding α,α-disubstituted unnatural α-amino ester derivatives were obtained in moderate to high yields (67–85%) with high enantioselectivities (up to 93% ee) under mild reaction conditions.

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