Institut Sciences Chimiques de Rennes, UMR 6226 CNRS-Université de Rennes 1, Catalyse et Organometalliques, Campus de Beaulieu, 35042 Rennes, France.
ChemSusChem. 2012 Aug;5(8):1559-67. doi: 10.1002/cssc.201100771. Epub 2012 Jul 25.
Solvent is one of the major sources of waste in the course of catalyzed direct arylations. Some palladium-catalyzed direct arylations of heteroaromatics can be advantageously performed without any solvent. In the presence of palladium catalysts (1 mol %) and potassium acetate as the base, the direct 5-arylation of some thiazoles, thiophenes, furans, or pyrroles with aryl bromides as coupling partners proceeds highly regioselectively and in moderate to high yields. However, the use of these solvent-free conditions is limited to electron-deficient aryl bromides.
溶剂是催化直接芳基化过程中主要的废物来源之一。一些钯催化的杂芳烃直接芳基化可以在没有任何溶剂的情况下有利地进行。在钯催化剂(1 摩尔%)和醋酸钾作为碱的存在下,芳基溴化物作为偶联试剂,一些噻唑、噻吩、呋喃或吡咯与芳基溴化物的直接 5-芳基化反应具有高度的区域选择性,中等至高产率。然而,这些无溶剂条件的使用仅限于缺电子的芳基溴化物。