Rh‐Catalyzed Direct Amination of Unactivated C(sp3)−H bond with Anthranils Under Mild Conditions |
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| Authors: | Conghui Tang Miancheng Zou Jianzhong Liu Xiaojin Wen Xiang Sun Yiqun Zhang Prof. Ning Jiao |
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| Affiliation: | 1. http://sklnbd.bjmu.edu.cn/nj/;2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China;3. (+86)?10‐82805297;4. State Key Laboratory of Elemento-organic Chemistry, Nankai University, Tianjin, China |
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| Abstract: | C?N Bond formation is of great significance due to the ubiquity of nitrogen‐containing compounds. Here, a mild and efficient RhIII‐catalyzed C(sp3)?H aryl amination reaction is reported. Anthranil is employed as the nitrogen source with 100 % atom efficiency. This C?H amination reaction exhibits broad substrate scope without using any external oxidants. Mechanistic studies including rhodacycle intermediates, H–D exchange, kinetic isotope effect (KIE) experiments, and in situ IR are presented. |
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| Keywords: | amination anthranils C− H activation heterocycles rhodium |
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