Zhang Jun, Wang Zhong, Chen Lingjuan, Liu Yan, Liu Ping, Dai Bin
School of Chemistry and Chemical Engineering, The Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Bingtuan, Shihezi University Shihezi City 832004 China
RSC Adv. 2018 Dec 12;8(72):41651-41656. doi: 10.1039/c8ra09367a. eCollection 2018 Dec 7.
The rapid and efficient KI/HO-mediated 2-sulfonylation of substituted indoles and -methylpyrrole was established. The corresponding 2-sulfonylation products are synthesized from readily available sulfur sources, namely arylsulfonyl hydrazides, 4-methylbenzenesulfinic acid and sodium 4-methylbenzenesulfinate in good to excellent yields in only 5 min. Moreover, the aqueous solution of hydrogen peroxide is used as both oxidant and solvent. Mechanistic studies demonstrated that 2,3-diiodoindoline was the main sulfonylation intermediate.
已建立了快速高效的碘化钾/过氧化氢介导的取代吲哚和N-甲基吡咯的2-磺酰化反应。相应的2-磺酰化产物由易于获得的硫源，即芳基磺酰肼、对甲苯亚磺酸和对甲苯亚磺酸钠合成，反应仅需5分钟，产率良好至优异。此外，过氧化氢水溶液用作氧化剂和溶剂。机理研究表明，2,3-二碘吲哚啉是主要的磺酰化中间体。
