Cu-catalyzed reductive aminomethylation of 1,3-dienes with N,O-acetals: facile construction of β-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.

Automated summary

A copper-catalyzed highly regio- and enantioselective reductive aminomethylation reaction has been reported for the first time, providing a convenient access to beta-chiral amines with all-carbon quaternary stereocenters, which are commonly found in pharmaceuticals and natural products. This method features good functional group tolerance, facile scalability, and easy derivatization of products to useful building blocks.