Visible-light-driven photocatalyst-free synthesis of N-aryl amino acids

Abstract

A visible-light-driven, three-component coupling for the synthesis of N-aryl amino acids and unnatural peptides is described, which proceeds under mild, catalyst- and photocatalyst-free conditions—even under natural sunlight. Glyoxylates, anilines, and 4-alkyl 1,4-dihydropyridines are efficiently assembled under mild conditions. This transformation exploits the intrinsic photoreactivity of 4-alkyl dihydropyridines, which directly generate alkyl radicals without external photocatalysts or electron–donor–acceptor (EDA) complexes. The reaction displays broad substrate scope, good functional-group tolerance, and excellent scalability, and enables late-stage modification of complex bioactive molecules.