Regio- and stereoselective tert-butylthiolation of internal alkynes with thioethers initiated and maintained by silylium-ion catalysis

硅鎓离子催化引发和维持的内炔与硫醚的区域选择性和立体选择性叔丁基硫代化反应

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Abstract

A two-component protocol for the regio- and trans-selective addition of aryl tertiary alkyl (especially tert-butyl) thioethers across internal C[triple bond, length as m-dash]C triple bonds is reported. This carbothiolation is initiated by the catalytic formation of a silylated sulfonium ion as a tertiary carbenium ion (tert-butyl cation) source. Competing loss of a proton by β-elimination of that carbenium-ion intermediate and as such a potential hydrothiolation pathway are efficiently suppressed by the substoichiometric addition of an arylsilane as a "proton-into-silylium ion" generator. Through this, the silylium-ion activation is restored, thereby maintaining the carbothiolation pathway. The method enables the synthesis of sterically crowded, fully substituted aryl vinyl sulfides as well as the sulfoxides and sulfones.

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