Cu-catalyzed reductive aminomethylation of 1,3-dienes with N,O-acetals: facile construction of beta-chiral amines with quaternary stereocenters

A copper-catalyzed highly regio- and enantioselective reductive aminomethylation of 1,1-disubstituted 1,3-dienes with N,O-acetals is reported for the first time. This work provides expedient access to beta-chiral amines with all-carbon quaternary stereocenters, motifs commonly found in pharmaceuticals and natural products. Moreover, this method features good functional group tolerance, facile scalability, and easy derivatization of products to useful building blocks.