Photo/Copper-CatalyzedOxidative Direct Diphosphorothiolationof Indolin-2-ones with P(O)SH Compounds
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Abstract
Abstract 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.
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Authors: Pengbo Zhang, Xinyi Guo, Mengke Yang, 蔡宜连, Longyu Wang, Yuzhen Gao
Institutions: Henan Medical University, Fujian Institute of Research on the Structure of Matter