Synthesis of β-amino acid derivatives via photoredox-catalyzed radical cross-coupling of anilines with diazo compounds

A photoredox-catalyzed radical cross-coupling protocol for the synthesis of beta-amino acid derivatives has been developed. Under mild reaction conditions, readily available N-methyl anilines and alpha-diazoacetates are used as radical precursors, and nitrogen gas is the only side product. This straightforward and atom-economic protocol enables the synthesis of a range of beta-amino acid esters in moderate to excellent yields (up to 96%). This work has not only provided a new and efficient strategy for the synthesis of beta-amino acid esters, but also settled the remaining challenges in radical transformation-based synthetic strategies for beta-amino acid derivatives.