Para-coupling of phenols with C2/C3-substituted benzothiophene S-oxides
Para-coupling of phenols with C2/C3-substituted benzothiophene S-oxides
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DOI：
10.1016/j.tet.2020.131315
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发表时间：
2020-12-18
期刊：
影响因子：
2.1
通讯作者：
Procter, David J.
中科院分区：
文献类型：
--
作者：
He, Zhen;Biremond, Tony;Procter, David J.
C2和C3取代的苯并噻吩是药物和材料化学中常见的结构。苯酚与苯并噻吩的交叉偶联是制备这些重要分子的有用途径。在这份报告中，我们揭示了一个有效的C-H/C-H型交叉偶联的苯并噻吩，活化为它们的S-氧化物，与苯酚，得到C2/C3芳基化苯并噻吩。尽管先前的报道描述了在酚和亚砜之间的邻位处的交叉偶联，但该程序允许通常使其邻位被封闭的酚的对位官能化。(C)2020爱思唯尔有限公司版权所有。
C2 and C3 substituted benzothiophenes are common structures in medicinal and materials chemistry. The cross-coupling of phenols with benzothiophenes is a useful route towards these important molecules. In this report we reveal an efficient C-H/C-H-type cross-coupling of benzothiophenes, activated as their S-oxides, with phenols to give C2/C3 arylated benzothiophenes. Whereas previous reports describe cross-coupling at the ortho-position between phenols and sulfoxides, this procedure allows para-functionalization of phenols that typically have their ortho positions blocked. (C) 2020 Elsevier Ltd. All rights reserved.