Enantioselective synthesis of 3-substituted tryptamines as core components of central nervous system drugs and indole natural products

Abstract

Application of the MacMillan iminium ion Michael and Friedel–Crafts type reactions to γ-amino α,β-unsaturated butanals led to the corresponding β-substituted butanals in good yields and high enantioselectivities. The products could be useful intermediates in the synthesis of indole-based central nervous system (CNS) drugs and natural products.