Chiral β-aryl (heteroaryl) alkylamines have been prepared from N-tosyl alkylaziridines via regiospecific nucleophilic ring opening and subsequent desulfonylation in good to excellent yields. The corresponding aziridines are easily obtained from commercially available (S)-α- amino acids, so this method is the first effective route to asymmetric β-aryl (heteroaryl) alkylamines.
