Fan-Lin Zeng, Jianan Chen, Yuxin Luo, Yanli Yin, Jinwei Yuan, Teck-Peng Loh
Introducing amino acids/peptides onto the heterocycle via photocatalytic methods remains a significant challenge. A novel visible-light-driven carbamoylation approach was first developed, facilitating the efficient synthesis of dibenzo[ b,f ][1,4]oxazepine carbonyl amino acid/peptide derivatives (>40 examples, up to 98% yield) from DHP-tagged amino acids/peptides. This strategy offers mild reaction conditions, easy scale-up, broad substrate compatibility, environmental friendliness, simple operation, and high tolerance to diverse functional groups. In addition, it enables late-stage functionalization of amine-containing drugs/natural products/proteins.