A simple method for the preparation of homochiral ring-substituted 1-aryl-2-aminopropanones 2(“cathinones”) is described, involving initial Friedel-Crafts acylation of aromatics with (S)- or (R)-N-trifluoroacetylalanyl chloride, followed by acid hydrolysis of the intermediate trifluoroacetamido intermediates 1, for which X-ray diffraction analysis confirmed the structures.