Shi Lei, Wang Min, Fan Chun-An, Zhang Fu-Min, Tu Yong-Qiang
Department of Chemistry & State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, P. R. China.
Org Lett. 2003 Sep 18;5(19):3515-7. doi: 10.1021/ol0353868.
[reaction: see text] A rapid and direct amination of aryl halides has been developed in good to high yields under microwave irradiation without a transition-metal catalyst. This reaction is a particularly powerful method for the coupling of electron-rich aryl halides with various amines. In some cases, the excellent regioselectivity could be observed, which facilitated the preparation of meta-substituted anilines from ortho- or para-substituted phenylhalides. In addition, a mechanism via the interesting benzyne intermediate has been proposed.
[反应：见正文] 在微波辐射下，无需过渡金属催化剂，已开发出一种能以良好至高产率实现芳基卤化物快速直接胺化的方法。该反应是使富电子芳基卤化物与各种胺进行偶联的一种特别有效的方法。在某些情况下，可以观察到优异的区域选择性，这有利于从邻位或对位取代的苯基卤化物制备间位取代的苯胺。此外，还提出了一种经由有趣的苯炔中间体的机理。
