We herein report an ammonium salt-catalyzed protocol for the regioselective ring opening of aryl-aziridines with β-keto esters. The reaction gives access to a variety of highly functionalized target molecules with two consecutive stereo-genic centers and can be rendered enantioselective (up to e.r. = 91:9) by using bifunctional chiral ammonium salt catalysts.
Keywords: Alkylation; Aziridine opening; Bifunctional ammonium salt; Organocatalysis; Regioselectivity.