A Base-Catalyzed Domino-Isomerization–Hydroamination Reaction—A New Synthetic Route to Amphetamines

An efficient synthesis of pharmaceutically interesting amphetamines by a base-catalyzed domino-isomerization–hydroamination reaction is presented. Starting from allylbenzene and various primary or secondary amines, the basic structural pattern of amphetamines is synthesized directly in yields of up to 91% in the presence of catalytic amounts of n-butyllithium.