An asymmetric and highly practical thiosulfinylation of alkynes is established for the synthesis of sultim derivatives. The disclosed platform featured broad substrate scope and group tolerance for diverse biologically important molecules under mild and operationally simple conditions. Notably, the obtained chiral sulfinyl derivatives have demonstrated their potential application in further gram-scale synthesis and product derivatizations, providing a chance for drug discovery.
View Article and Find Full Text PDFA thermoinduced radical homolytic substitution cyclization of alkenyl tethered sulfinate esters was displayed under mild metal-free conditions, enabling the functionalization of alkenes and leading to structurally diverse value-added sultine products. The process utilizes readily available substrates using inexpensive 5% benzoyl peroxide (BPO) as an initiator to generate functionalized sultines with broad functional group tolerance in medium to excellent yields in a highly atom-economical manner. In addition, the obtained sultines could be further readily functionalized toward valuable sultone frameworks in one pot.
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