Photoredox-catalyzed three-component alkylation of glycine derivatives and peptides via a site-selective 1,5-hydrogen atom transfer cascade†

We report a visible-light-mediated three-component reaction via N-centered radical-mediated 1,5-hydrogen atom transfer combined with site-selective remote C(sp³)–H cross-coupling reactions of alkenes with alkyl radicals for the α-C(sp³)–H alkylation of glycine derivatives and peptides. This protocol performs the double functionalization of alkenes and provides a promising alternative route for the modular synthesis of peptide-derived bioactive compounds. Additionally, the potential synthetic value of this transformation is demonstrated in the scale-up reactions and late-stage functionalization of peptides.