Palladium-catalyzed method for arene pyridination in pharmaceuticals, suggesting high functional group tolerance.
We report a palladium-catalyzed cross-coupling of arylthianthrenium and pyridylphosphonium salts for direct arene pyridination. The silver-mediated transformation forges aryl-pyridine bonds exclusively at pyridine C4 under mild conditions without directing groups. This strategy combines two bench-stable reagents, circumventing limitations associated with conventional pyridination precursors. With excellent functional group tolerance, the method establishes a versatile platform for late-stage aromatic diversification in pharmaceutical research, as demonstrated through successful modification of complex bioactive scaffolds.
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Yue et al. (2025) studied this question.
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