Copper-Catalyzed Carboxamide-Directed Ortho Amination of Anilines with Alkylamines at Room Temperature
Copper-Catalyzed Carboxamide-Directed Ortho Amination of Anilines with Alkylamines at Room Temperature
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DOI：
10.1021/ol500464x
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发表时间：
2014-03-21
期刊：
影响因子：
5.2
通讯作者：
Chen, Gong
中科院分区：
文献类型：
--
作者：
Li, Qiong;Zhang, Shu-Yu;Chen, Gong
在这份报告中，一个高效的方法，通过铜催化的羧酰胺定向胺化与烷基胺的苯胺邻位上的烷基氨基基序的室温安装。这种方法提供了一个实用的解决方案，从简单的起始材料的复杂的芳胺的快速合成，并使新的规划策略的建设芳胺含药效团。提出了单电子转移（SET）介导的机理。
In this report, a highly efficient method for the room temperature installation of alkyl amino motifs onto the ortho position of anilines via Cu-catalyzed carboxamide-directed amination with alkylamines is described. This method offers a practical solution for the rapid synthesis of complex arylamines from simple starting materials and enables new planning strategies for the construction of arylamine-containing pharmacophores. A single electron transfer (SET)-mediated mechanism is proposed.