Sulfones are key motifs in pharmaceuticals, agrochemicals, and functional materials, as well as versatile intermediates in synthesis. We report a general and practical protocol for sulfone synthesis that combines the group-transfer capability of hypervalent iodine reagents (HIRs)—particularly in situ-generated sulfonyl-containing HIRs—with organozinc pivalates. The method delivers a broad range of sulfones in high yields under mild conditions, exhibiting excellent functional group tolerance. Importantly, the method enables efficient sulfonylation using sodium bicyclo1.1.1pentane sulfinate (BCP–SO2Na), providing streamlined access to functionalized BCP-sulfones. The protocol further enables in situ sulfinate generation and one-pot transformations. These findings expand the scope of HIR-enabled umpolung reactivity and offer a practical, modular and operationally simple platform for accessing sulfones with broad synthetic and medicinally relevance.
Cunha et al. (Thu,) studied this question.