Palladium-CatalyzedSite-Selective C–H Sulfonylationvia Aryl Thianthrenium Salts to Access Diarylsulfones

We presented a highly efficient palladium-catalyzed site-selective C–H sulfonylation reaction via aryl thianthrenium salts. By utilizing readily available and cost-effective arenes along with sodium sulfinates, we achieved the C(sp²)–S cross-coupling with high efficiency, establishing a dependable method for synthesizing diarylsulfones with satisfactory yields. This method exhibits excellent tolerance toward functional groups, scalability, and the synthesis or late-stage functionalization of bioactive molecules, making it a valuable sulfonylation tool for drug modifications.