Direct catalytic enantioselective α-aminomethylation of ketones

Abstract

(Chemical equation presented). A proline-catalyzed Mannich reaction produces α-aminomethylated ketones in high yield and with excellent ee values (see scheme). The Mannich bases resulting from this highly practical one-pot three-component asymmetric reaction are of particular interest, for example, as synthetic building blocks and precursors of pharmaceutically valuable 1,3-amino alcohols.