| Natural scaffolds-inspired synthesis of CF3-substituted macrolides enabled by Rh-catalyzed C–H alkylation macrocyclization |
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| 作者姓名： | Tongyu Bi Yi Xu Xin Xu Bixi Tang Qing Yang Yi Zang Zhenyang Lin Jia Li Weibo Yang |
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| 作者单位： | 1. Chinese Academy of Sciences Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences;2. University of Chinese Academy of Sciences;3. Department of Chemistry, The Hong Kong University of Science and Technology;4. School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences;5. Open Studio for Druggability Research of Marine Natural Products, Pilot National Laboratory for Marine Science and Technology (Qingdao) |
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| 摘 要： | The development of innovative strategies and methods to provide natural product-like macrocycles not accessible by biosynthesis, but endowed with novel bioactivities and simplified structure, is highly desirable. Inspired by the key scaffolds of rapamycin and FR252921, herein, we report a Rh（III）-catalyzed C–H alkylation macrocyclization, which enables access to CF3-substituted macrolides. DFT calculations reveal that the chemoselectivity between C–H alkylation and olefination macrocyclization w...
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| 收稿时间： | 2021-07-17 |
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