Visible-light mediated synthesis of bicalutamide by regioselective hydroxysulfonylation of acrylamides
Mercedes Zurro, Sergio Torres-Oya, Estíbaliz Merino*
Eur. J. Org. Chem. 2023, Accepted Articles
|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.