An efficient synthesis of substituted 1,4-diazepines by a Pd catalyzed amination and sequential hydrogenation condensation |
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| Authors: | Xiao-Jian Wang Yu-Lin Tian Qing-Yang Zhang Jian-Guo Qi Da-Li Yin |
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| Institution: | State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China |
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| Abstract: | An efficient synthesis of substituted 1,4-diazepines is developed. The accessible intermediates have been obtained via Pd-catalyzed amination. The subsequent hydrogenation and intramolecular condensation sequences could be conducted successively in one pot without special operation. The mild and general strategy enables the synthesis of various substituted 1,4-diazepines in high yields. |
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| Keywords: | 1 4-Diazepines Pd-catalyzed amination Hydrogenation Intramolecular condensation |
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