Silver(I)-catalyzed and DBU-promoted isomerization/addition of propargyl alcohols to amines to access β-aminoketones

Abstract

An alternative strategy for the synthesis of β-aminoketones have been achieved through silver(I)-catalyzed and DBU-promoted isomerization/addition of propargyl alcohols to amines. The mechanism likely involves an isomerization and sequential addition combined with the alkenyl radical process. This protocol features broad substrate scope, superior atom economy, operational simplicity, and good to excellent yields, and provides a new method for the synthesis of drug Proroxan on gram-scale, presenting a practical application for the construction of β-aminoketones.