Rh-Catalyzed Cascade C–H Functionalization/Aromatization of Benzylamines with Vinylcyclopropanes: Access to Functionalized Isoquinolines

A Rh-catalyzed sequential site-selective C-H functionalization, allylation, and annulation of benzylamines with vinylcyclopropane (VCP) has been accomplished to furnish functionalized isoquinolines. In this reaction cascade, amine is oxidized to imine and acts as a directing group to achieve the site-selective C-H functionalization utilizing VCP as the coupling partner. The utilization of simple substrates, substrate scope, step/atom economy, functional group tolerance, and postsynthetic transformations are the important practical features.