2023
DOI: 10.1002/ejoc.202300535
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Visible‐Light‐Mediated Synthesis of Bicalutamide by Regioselective Hydroxysulfonylation of Acrylamides

Abstract: Synthesis of anticancer drug bicalutamide promoted by visible light in one step from the corresponding N‐arylacrylamide is described. This approach involves a one‐pot hydroxysulfonylation reaction via a photocatalytic redox process. The use of Na2Eosin Y as photocatalyst and blue light allows the access to a broad range of α‐hydroxysulfonylamides bearing a quaternary center in moderate to good yields with complete regioselectivity via radical process.

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