Title | N-Trifluoropropylation of Azoles through N-Vinylation and Sequential Hydrogenation |
Author | |
Publication Years | 2022-11-18
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DOI | |
Source Title | |
ISSN | 0022-3263
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EISSN | 1520-6904
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Volume | 87Issue:22Pages:15703-15712 |
Abstract | Installing a fluoroalkyl group onto the nitrogen atom of azoles represents a potential strategy for lead optimization in medicinal chemistry. Herein, we describe a method for the N-trifluoropropylation of azoles. This process is accomplished using a combination of regioselective N-vinylation and sequential hydrogenation. The two-step sequence is applicable to a diverse set of azoles and tolerates a wide range of functionalities. In addition, we showcase its practicability and utility through the gram-scale synthesis and the late-stage modification of a complex molecule. |
URL | [Source Record] |
Indexed By | |
Language | English
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SUSTech Authorship | Others
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WOS Accession No | WOS:000882962300001
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ESI Research Field | CHEMISTRY
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Scopus EID | 2-s2.0-85141997033
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Data Source | Scopus
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Citation statistics |
Cited Times [WOS]:3
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Document Type | Journal Article |
Identifier | http://kc.sustech.edu.cn/handle/2SGJ60CL/416490 |
Department | Southern University of Science and Technology |
Affiliation | 1.School of Chemistry and Chemical Engineering,Guangzhou University,Guangzhou,510006,China 2.State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University,Guiyang,550014,China 3.Guangdong Provincial Key Laboratory of Catalysis,Southern University of Science and Technology,Shenzhen,518055,China |
Recommended Citation GB/T 7714 |
Chen,Shu Jie,Li,Jia Hui,He,Zhi Qing,et al. N-Trifluoropropylation of Azoles through N-Vinylation and Sequential Hydrogenation[J]. JOURNAL OF ORGANIC CHEMISTRY,2022,87(22):15703-15712.
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APA |
Chen,Shu Jie.,Li,Jia Hui.,He,Zhi Qing.,Chen,Guo Shu.,Zhuang,Yin Yin.,...&Liu,Yun Lin.(2022).N-Trifluoropropylation of Azoles through N-Vinylation and Sequential Hydrogenation.JOURNAL OF ORGANIC CHEMISTRY,87(22),15703-15712.
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MLA |
Chen,Shu Jie,et al."N-Trifluoropropylation of Azoles through N-Vinylation and Sequential Hydrogenation".JOURNAL OF ORGANIC CHEMISTRY 87.22(2022):15703-15712.
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