Pd-catalyzed process improves yields of N-arylated sulfoximines in gram-scale synthesis, suggesting wider applications.
We report a Pd/BrettPhos-catalyzed denitrative C–N cross-coupling of NH-sulfoximines and nitroarenes, which directly delivers diverse N-arylated sulfoximines in good yields with broad functional group tolerance. By using inexpensive nitroarenes as electrophiles, the protocol avoids comparatively costly haloarenes and streamlines the synthesis. The use of catalytic amount of aluminum triflate significantly enhances the yields and facilitates the reaction under Pd/NHC catalysis. Successful application to pharmaceutical analog synthesis and gram-scale reactions highlights the practicality of the protocol.
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Yang et al. (2025) studied this question.
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