Fine Nathel Noah F, Kim Junyong, Hie Liana, Jiang Xingyu, Garg Neil K
Department of Chemistry and Biochemistry, University of California , Los Angeles, California 90095, United States.
ACS Catal. 2014 Sep 5;4(9):3289-3293. doi: 10.1021/cs501045v. Epub 2014 Aug 20.
The nickel-catalyzed amination of aryl -sulfamates and chlorides using the green solvent 2-methyl-THF is reported. This methodology employs the commercially available and air-stable precatalyst NiCl(DME), is broad in scope, and provides access to aryl amines in synthetically useful yields. The utility of this methodology is underscored by examples of gram-scale couplings conducted with catalyst loadings as low as 1 mol % nickel. Moreover, the nickel-catalyzed amination described is tolerant of heterocycles and should prove useful in the synthesis of pharmaceutical candidates and other heteroatom-containing compounds.
报道了使用绿色溶剂2-甲基四氢呋喃进行镍催化的芳基磺酸酯和氯化物的胺化反应。该方法采用市售且对空气稳定的预催化剂NiCl(DME)，适用范围广，能以合成上有用的产率得到芳基胺。以低至1 mol%镍的催化剂负载量进行克级偶联的实例突出了该方法的实用性。此外，所描述的镍催化胺化反应对杂环具有耐受性，在药物候选物和其他含杂原子化合物的合成中应会很有用。
