Construction of α-Acyl-β-amino Amides via Multicomponent Reactions of β-Acyloxy Alkenyl Amides with Amines and Aldehydes

Herein, we describe a novel multicomponent synthesis of α-acyl-β-amino amides with structural diversity and brevity from aldehydes, amines, and β-acyloxy alkenyl amides (AAAs). In this multicomponent protocol involving fragmentation and reassembly processes, AAAs act as the key building blocks for the construction of the β-amino amides simply via acid promotion, providing a step- and atom-economical approach to access these useful products with excellent diastereoselectivity.