Transition-Metal-Free Selective C@H Benzylation of Tertiary Arylamines by a Dearomatization-Aromatization Sequence
Transition-Metal-Free Selective C@H Benzylation of Tertiary Arylamines by a Dearomatization-Aromatization Sequence
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通过脱芳构化-芳构化序列对叔芳胺进行无过渡金属选择性 C-H 苄基化
DOI：
10.1002/chem.201803211
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发表时间：
2018
期刊：
影响因子：
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通讯作者：
Peng-Fei Xu
中科院分区：
文献类型：
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作者：
Guo-Qiang Xu;Zhi-Tao Feng;Ji-Tao Xu;Zhu-Yin Wang;Yong Qin;Peng-Fei Xu
由于杂交系统在药物发现中的重要性，迫切需要将多种生物活性成分组装成单个分子。在这里，我们报告了叔芳胺的一般无过渡金属选择性C-H苄基化，在温和条件下具有良好至优异的产率，具有广泛的底物范围和高官能团耐受性。除芳胺化合物外，其它苯衍生物也可通过该方法合成相应的二芳基甲烷衍生物。一系列的控制实验和理论计算表明，该反应是一个脱芳构化-芳构化过程。
Due to the significance of hybrid systems in drug discovery, there is an urgent need to assemble multiple biologically active ingredients into a single molecule. Here, we report a general transition‐metal‐free selective C−H benzylation of tertiary arylamines in good to excellent yields with a broad substrate scope and high functional‐group tolerance under mild conditions. Besides arylamines, some other benzene derivatives also readily furnished the corresponding diaryl methane derivatives with this protocol. A series of control experiments and theoretical calculations indicated that this transition‐metal‐free reaction is a dearomatization‐aromatization process.