Pd(II)-Catalyzed Direct Sulfonylation of Unactivated C(sp³)–H Bonds with Sodium Sulfinates

A Pd­(II)-catalyzed sulfonylation of unactivated C­(sp3)–H bonds with sodium arylsulfinates using an 8-aminoquinoline auxiliary is described. This reaction demonstrates excellent functional group tolerance with respect to both the caboxamide starting material and the sodium arylsulfinate coupling partner, affording a broad range of aryl alkyl sulfones. Moreover, the late-stage modification of complex molecules was achieved via this sulfonylation protocol.