Demonstrates enhanced C–H functionalization in benzylamines, highlighting practical synthetic features.
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.
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Kumar et al. (2026) studied this question.
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