Diversification of Aryl Sulfonyl Compounds through Ligand‐Controlledmeta‐ andpara‐C−H Borylation

Abstract

AbstractAryl sulfones and aryl sulfonamides are of great importance in organic synthesis and medicinal chemistry. Althoughortho‐C−H functionalization of aryl sulfonyl compounds has been extensively explored, the functionalization of remotemeta‐andpara‐C−H bonds is very rare. Herein, we report a tunablemeta‐andpara‐selective C−H borylation of aryl sulfonyl compounds enabled by computationally designed ligands and iridium catalyst. This method is capable of accommodating a broad range of substrates under mild reaction conditions. Gram‐scale preparation can be achieved with iridium catalyst loading as low as 0.1 mol%. As the introduced boronate group can be easily converted into many other groups, our method provides a general solution to installing functional groups at eithermeta‐ orpara‐position of aryl sulfones and aryl sulfonamides with good to excellent selectivity.