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Construction of C2-Spirocyclopropyl-Indolin-3-Ones through Base-Promoted [2+1] Annulation Reaction of Indolin-3-ones with Bromosulfonium Salts |
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| Authors: | Mao Zhang Fenfen Yang Xiang Guan Mingshan Shuai Qingqing Zhang Prof. Xiaozhong Fu Prof. Yuanyong Yang Prof. Meng Zhou Prof. Bin He Prof. Yonglong Zhao |
| Affiliation: | 1. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China These authors contributed equally to this work. Contribution: Writing - original draft (equal);2. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China These authors contributed equally to this work. Contribution: Writing - review & editing (equal);3. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China Contribution: Formal analysis (supporting);4. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China Contribution: Methodology (supporting);5. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China Contribution: Methodology (supporting), Supervision (supporting);6. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China Contribution: Methodology (supporting), Software (supporting);7. School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, 550004 P. R. China |
| Abstract: | A simple base-promoted [2+1] annulation of indolin-3-ones and bromosulfonium salts has been developed in this article. This strategy uses simple and easily prepared indolin-3-ones 1 as C1 synthons and bromosulfonium salts 2 as C2 synthons under mild reaction conditions, and 33 examples of C2-spirocyclopropyl-indolin-3-ones were obtained with up to 99 % yield and >20 : 1 dr. |
| Keywords: | [2+1] annulation bromosulfonium salts indolin-3-ones C2-spirocyclopropyl-indolin-3-ones |