An additive-free, visible light-driven annulation between -aryl amino acids and maleimide to form tetrahydroquinolines (THQs) is disclosed. Photochemical activation of an electron donor-acceptor (EDA) complex between amino acids and maleimides drives the reaction, and aerobic oxygen acts as the terminal oxidant in the net oxidative process. A range of -aryl amino acids and maleimides have been investigated as substrates to furnish the target THQ in good to excellent yield. Mechanistic investigations, including titration and UV-vis studies, demonstrate the key role of the EDA complex as the photoactive species.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9830629PMC
http://dx.doi.org/10.1021/acs.joc.2c02448DOI Listing

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