Photo/Copper-Catalyzed Oxidative Direct Diphosphorothiolation of Indolin-2-ones with P(O)SH Compounds

A visible-light-promoted cross-dehydrogenative coupling (CDC) of indolin-2-ones with S-hydrogen phosphorothioates via 4H elimination has been developed, providing 3,3-diphosphorothiolated oxindoles in good yields with broad functional group tolerance. The protocol was also extended to monophosphorothiolation and late-stage diversification of drug-derived substrates. Notably, the products displayed potent and selective butyrylcholinesterase (BuChE) inhibitory activity, suggesting potential as leads for Alzheimer's disease.