Backbone-enabled modification of peptides with benzoquinone via palladium-catalyzed δ-C(sp2)–H functionalization

Abstract

Backbone-enabled site-selective modification of peptides with benzoquinone via Pd-catalyzed δ-C(sp²)–H functionalization has been achieved. The amide groups of peptides serve as internal directional groups, facilitating C–H functionalization through a kinetically less favored six-membered palladacycle. This methodology presents novel opportunities for the late-stage site-selective diversification of peptides.