School of Pharmaceutical and Materials Engineering & Institute for Advanced Studies, Taizhou University, 1139 Shifu Avenue, Taizhou 318000, China.
Chem Commun (Camb). 2021 Jan 28;57(7):915-918. doi: 10.1039/d0cc07632e.
A convenient and efficient approach to (E)-alkylsulfonyl olefins via a metal/light-free three-component reaction of alkenylboronic acids, sodium metabisulfite and Katritzky salts is described. This alkylsulfonylation proceeds smoothly with a broad substrate scope, leading to diverse (E)-alkylsulfonyl olefins in moderate to good yields. During the process, excellent functional group tolerance is observed and sodium metabisulfite is used as the source of sulfur dioxide. Mechanistic studies show that the alkyl radical generated in situ from Katritzky salt via a single electron transfer with alkenylboronic acid or DIPEA is the key step for providing an alkyl radical intermediate, which undergoes further alkylsulfonylation with sulfur dioxide.
一种方便、高效的方法,用于通过金属/无光照的三组分反应,将烯基硼酸、亚硫酸氢钠和 Katritzky 盐转化为(E)-烷基磺酰基烯烃。这种烷基磺酰化反应具有广泛的底物范围,以中等至良好的收率得到各种(E)-烷基磺酰基烯烃。在反应过程中,观察到了优异的官能团耐受性,并且亚硫酸氢钠被用作二氧化硫的来源。机理研究表明,Katritzky 盐通过与烯基硼酸或 DIPEA 的单电子转移原位生成的烷基自由基是提供烷基自由基中间体的关键步骤,该中间体进一步与二氧化硫发生烷基磺酰化反应。