A new convenient approach to chiral β-aryl(heteroaryl)alkylamines

Chiral beta -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)-alpha -amino acids. so this method is the first effective route to asymmetric beta -aryl(heteroaryl)alkylamines. (C) 2001 Elsevier Science Ltd. All rights reserved.