A method for enantioselective direct aamination reaction catalyzed by a sterically "frustrated" Lewis acid/Bronsted base complex is disclosed. Cooperative functioning of the Lewis acid and Bronsted base components gives rise to in situ enolate generation from monocarbonyl compounds. Subsequent reaction with hydrogen-bond activated dialkyl azodicarboxylates delivers alpha-aminocarbonyl compounds in high enantiomeric purity.