Department of Organic Chemistry, Kaunas University of Technology, Radvilėnų pl. 19, LT-50254 Kaunas, Lithuania.
Univ. Artois, CNRS, Centrale Lille, Univ. Lille, UMR 8181-UCCS-Unité de Catalyse et Chimie du Solide, F-62300 Lens, France.
Molecules. 2021 Nov 11;26(22):6822. doi: 10.3390/molecules26226822.
Cu-catalyzed -arylation is a useful tool for the chemical modification of aromatic heterocycles. Herein, an efficient carbon-nitrogen cross-coupling of methyl 3-amino-1-benzothiophene-2-carboxylate with a range of (hetero)aryl iodides using CuI, l-proline and CsCO in dioxane at moderate temperature is described. The procedure is an extremely general, relatively cheap, and experimentally simple way to afford the -substituted products in moderate to high yields. The structures of the new heterocyclic compounds were confirmed by NMR spectroscopy and HRMS investigation.
铜催化的芳基化是一种用于芳香杂环化学修饰的有用工具。在此，我们描述了一种使用碘化亚铜、l-脯氨酸和碳酸铯在二氧六环中于中等温度下高效实现 3-氨基-1-苯并噻吩-2-羧酸甲酯与一系列（杂）芳基碘化物的碳氮交叉偶联的方法。该方法具有极高的通用性、相对较低的成本和实验操作的简便性，可中等至高收率得到 -取代产物。新杂环化合物的结构通过 NMR 光谱和高分辨质谱（HRMS）确证。
