Regioselective Metal- and Reagent-Free Arylation of Benzothiophenes by Dehydrogenative Electrosynthesis
Regioselective Metal- and Reagent-Free Arylation of Benzothiophenes by Dehydrogenative Electrosynthesis
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DOI：
10.1002/anie.201808555
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发表时间：
2018-10-01
影响因子：
16.6
通讯作者：
Waldvogel, Siegfried R.
中科院分区：
文献类型：
--
作者：
Lips, Sebastian;Schollmeyer, Dieter;Waldvogel, Siegfried R.
报道了一种合成苯并噻吩和苯酚组成的联芳化合物的新方法。这些杂联芳基化合物在制药、生物和高性能光电应用中具有极大的意义。所述无金属和试剂的、电合成的和高效的方法使得能够以区域选择性方式生成2-和3-（羟基苯基）苯并[B]噻吩。所描述的一步合成易于进行、可扩展且固有安全。产物以高达88%的高产率和高选择性提供。该反应的特点是反应范围广，可接受多种官能团。
A novel strategy for the synthesis of biaryls consisting of a benzothiophene and a phenol moiety is reported. These heterobiaryls are of utmost interest for pharmaceutical, biological, and high-performance optoelectronic applications. The metal- and reagent-free, electrosynthetic, and highly efficient method enables the generation of 2- and 3-(hydroxyphenyl)benzo[b]thiophenes in a regioselective fashion. The described one-step synthesis is easy to conduct, scalable, and inherently safe. The products are afforded in high yields of up to 88% and with exquisite selectivity. The reaction also features a broad scope and tolerates a large variety of functional groups.