Rapid Synthesis of Fused N-Heterocycles by Transition-Metal-Free Electrophilic Amination of Arene C-H Bonds
Rapid Synthesis of Fused N-Heterocycles by Transition-Metal-Free Electrophilic Amination of Arene C-H Bonds
复制标题
DOI：
10.1002/anie.201309973
复制
发表时间：
2014-03-03
影响因子：
16.6
通讯作者：
Kuerti, Laszlo
中科院分区：
文献类型：
--
作者：
Gao, Hongyin;Xu, Qing-Long;Kuerti, Laszlo
我们公开了一种有效的和操作简单的方案，用于在温和条件下从容易获得的2-硝基联芳基和PhMgBr开始制备稠合的N-杂环。用这种方法已经合成了二十多个N-杂环化合物，其中包括两个具有生物活性的天然产物。通过密度泛函理论计算，提出了芳香环化反应的分步亲电机理。
We disclose an efficient and operationally simple protocol for the preparation of fused N-heterocycles starting from readily available 2-nitrobiaryls and PhMgBr under mild conditions. More than two dozen N-heterocycles, including two bioactive natural products, have been synthesized using this method. A stepwise electrophilic aromatic cyclization mechanism was proposed by DFT calculations.