Copper-Catalyzed Electrophilic Amination of Arylboronic Acids with Anthranils: An Access to <i>N</i>-Aryl-2-aminophenones
作者:Yang Gao、Simin Yang、Yibiao Li、Yanping Huo、Zongyi Huang、Zumin Chen、Xiao-Qiang Hu
DOI:10.1021/acs.joc.0c01109
日期:2020.8.7
An efficient copper-catalyzed electrophilic amination strategy has been established for the rapid synthesis of N-aryl-2-aminophenones from readily available arylboronic acids/esters and anthranils. This protocol features good functional group tolerance, broad substrate scope, and operational simplicity. Moreover, a tandem C–H borylation and C–N coupling protocol has also been developed to transform
已经建立了一种有效的铜催化亲电胺化策略,用于从容易获得的芳基硼酸/酯和蒽基快速合成N-芳基-2-氨基苯酮。该协议具有良好的功能组耐受性,广泛的底物范围和操作简便性。此外,还开发了串联的C–H硼化和C–N偶联方案,以将简单的芳烃转化为一锅中有价值的N-芳基-2-氨基苯酮。另外,通过合成各种有用的N-杂环和衍生物进一步证明了该方法的合成潜力。