N-Methoxy arenesulfonamide as a Sulfonyl Equivalent For Palladium-Catalyzed Sulfonylation of Arenes Through C-H Activation

The prevalence of sulfones in natural products, pharmaceutically active molecules and functional materials draw immense attention for their synthesis. Here, we report a palladium-catalyzed protocol for synthesizing diaryl sulfones from the arenes through C-H activation. N-methoxy arenesulfonamide was exploited as a potential sulfonyl donor by the cleavage of S-N bond through a radical pathway. The present methodology has several advantages: a simple, readily available catalytic system; the use of a stable sulfonyl donor; a relatively moderate excess of arene coupling partner for an undirected C-H activation process, along with the tolerances of aryl bromides and iodides, which in turn permits further cross-coupling reactions to afford cross-coupled sulfones.

Automated summary

This method utilizes palladium catalysis to synthesize diaryl sulfones from arenes, using N-methoxy arenesulfonamide as a sulfonyl donor, with advantages such as a simple and readily available catalytic system, stable sulfonyl donor, and tolerances of aryl bromides and iodides for further cross-coupling reactions to produce cross-coupled sulfones.