Benzylamines belong to an important class of building blocks in the synthesis of biologically active natural products and drugs. Encumbered by amide-directed -C-H activation, remote -selective C-H functionalization of benzylamines has hitherto not been realized to date. Here, we report a palladium-catalyzed -selective C-H olefination and acetoxylation of benzylamines using a functionalized benzoyl template. Enhancing the coordination strength of the directing group in the template significantly improved the site selectivity of C-H functionalization.
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