Recent applications of vinyl sulfone motif in drug design and discovery

Catalyst-Free Electrochemical Sulfonylation of Organoboronic Acids

“…32 White solid, 38 mg, 78% yield. 1 H NMR (500 MHz, CDCl 3 ): δ 7.81 (d, J = 8.5 Hz, 4H), 7.28 (d, J = 8.0 Hz, 4H), 2.39 (s, 6H). 13 C{ 1 H} NMR (125 MHz, CDCl 3 ): δ 143.9, 139.1, 129.8, 127.5, 21.5.…”

“…32 White solid, 27 mg, 51% yield. 1 4,4′-Sulfonylbis(chlorobenzene) (3z). 37a White solid, 32 mg, 55% yield.…”

“…So far, some diaryl sulfone-containing molecules have been successfully used in medical and commercial applications, such as dapsone, SR 33805 oxalate, and CX157 (Figure ). , In addition, the sulfone moiety is an important synthetic target and widely used as a versatile synthetic intermediate for organic chemistry. Therefore, many synthetic methodologies have been developed for the preparation of sulfones, for example, oxidation of sulfides, Friedel-Crafts-type sulfonation with sulfonyl halides, and coupling of sulfinic acid salts. − …”

Water-mediated radical C–H tosylation of alkenes with tosyl cyanide

“…Vinyl sulfone is a privileged structural motif in medicinal chemistry for drug discovery as well as a key structural unit in numerous of biologically active molecules. 1 The vinyl sulfone motif has been used particularly in the design of chemotherapeutics and neuroprotectives, as well as radioprotective agents. 2 Vinyl sulfones also efficiently act as Michael acceptors and 2π partners in cycloaddition reactions in synthetic chemistry.…”

“…1 The vinyl sulfone motif has been used particularly in the design of chemotherapeutics and neuroprotectives, as well as radioprotective agents. 2 Vinyl sulfones also efficiently act as Michael acceptors and 2π partners in cycloaddition reactions in synthetic chemistry. 3 Due to the importance of vinyl sulfones, continuous efforts have been devoted to using alkynes, α,β-unsaturated carboxylic acids, vinyl halides, terminal epoxides, oxime acetates, and tosylhydrazones as substrates.…”