Lead discovery of α,β-Unsaturated sulfones from a combinatorial library as inhibitors of inducible VCAM-1 expression

Copper-Catalyzed Difunctionalization of Allenes with Sulfonyl Iodides Leading to (E)-α-Iodomethyl Vinylsulfones

“…Vinylsulfone-containing compounds have been found to be widespread in biological molecules, such as cysteine protease inhibitors, HIV-1 inhibitors, covalent protease inhibitors, and inhibitors of a transpeptidase required for cell wall protein anchoring and virulence in Staphylococcus aureus . The difunctionalization of allenes through the halosulfonylation of allenes represents a particularly useful contribution to vinylsulfone-containing molecule synthesis because both the allylic halide and vinylsulfone moieties in the resulting α-halomethyl vinylsulfones can be further used as versatile building blocks in synthetic organic chemistry and transformed into high-value vinylsulfone-containing chemicals. , They also possess great synthetic potential due to the presence of a halo group.…”

Recent progress in the electrochemical selenofunctionalization of alkenes and alkynes

“…Selenovinyl sulfones are valuable synthetic intermediates 32 and display a wide range of biological and pharmacological activities. 33 Therefore, a plethora of synthetic strategies have been developed to synthesize these compounds. 34 In 2020, Xu, Chen and co-workers developed an electrosynthesis method for β-selenovinyl sulfones via selenosulfonylation of alkynes with sulfonyl hydrazines and diphenyl diselenide (Scheme 9).…”

Photo-induced stereo- and regiospecific sulfonylation of C–C multiple bonds exploiting the dual reactivity of sulfonium iodate(i) species

“…1). Besides displaying prominent biological activities 6–9 and promising abilities as a covalent warhead pharmacophore in drug discovery, 10 vinyl-sulfones serve as powerful chemical tools for constructing diverse complex structures and renowned materials. 11…”