| Diastereoselective 2,3-diazidation of indoles via copper(Ⅱ)-catalyzed dearomatization |
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| 作者姓名： | Jiang Liu Zhongjin Fang Xin Liu Yandong Dou Jianze Jiang Fangfang Zhang Jiaojiao Qu Qing Zhu |
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| 作者单位： | Key Laboratory of Bioorganic Synthesis of Zhejiang Province;Zhejiang Zhong Cheng Medicine Co. |
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| 基金项目： | the National Natural Science Foundation of China(Nos.21472172,21272212);Natural Science Foundation of Zhejiang Province(No.LY17B060009)。 |
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| 摘 要： | The copper-catalyzed directed dearomatization of indoles with the assistance of directing groups has been developed for the synthesis of 2,3-diazido indolines with good yields and excellent diastereoselectivities in aqueous solution.The resultant 2,3-diazides can be smoothly converted to other functional groups,including vicinal diamines,triazoles and benzotriazoles,in a single step.
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| 关 键 词： | Indole DIASTEREOSELECTIVE DEAROMATIZATION 2 3-Diazidation INDOLINE |
| 收稿时间： | 14 September 2019 |
Diastereoselective 2,3-diazidation of indoles via copper(II)-catalyzed dearomatization |
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| Jiang Liu,Zhongjin Fang,Xin Liu,Yandong Dou,Jianze Jiang,Fangfang Zhang,Jiaojiao Qu,Qing Zhu.Diastereoselective 2,3-diazidation of indoles via copper(II)-catalyzed dearomatization[J].Chinese Chemical Letters,2020,31(5):1332-1336. |
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| Institution: | 1. Department of Pharmaceutical and Biological Engineering, School of Chemical Engineering, Sichuan University, Chengdu, China;2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China |
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| Abstract: | The copper-catalyzed directed dearomatization of indoles with the assistance of directing groups has been developed for the synthesis of 2,3-diazido indolines with good yields and excellent diastereoselectivities in aqueous solution. The resultant 2,3-diazides can be smoothly converted to other functional groups, including vicinal diamines, triazoles and benzotriazoles, in a single step. |
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| Keywords: | Indole Diastereoselective Dearomatization 2 3-Diazidation Indoline |
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