Sulfonylation\nof Pyridyl Phosphonium Salts with Sulfinate\nSalts in Aqueous Media for the Synthesis of 4‑Pyridyl Sulfones\nvia C–P Bond Cleavage

A Na<sub>2</sub>S<sub>2</sub>O<sub>8</sub>-initiated\nsulfonylation\nof pyridyl phosphonium salts with sulfinate salts in aqueous media\nhas been developed for facile access to 4-pyridyl sulfones. The reactions,\nwhich employed pyridyl phosphonium salts as efficient pyridylation\nagents via C–P bond activation, showed both broad substrate\ngenerality and good functional group compatibility. In addition, the\nscale-up synthesis and the late-stage modification of pharmaceutically\nactive complex molecules (e.g., loratadine, bisacodyl) could also\nbe successfully realized.