中文版 | English
Title

N-Trifluoropropylation of Azoles through N-Vinylation and Sequential Hydrogenation

Author
Publication Years
2022-11-18
DOI
Source Title
ISSN
0022-3263
EISSN
1520-6904
Volume87Issue: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
SUSTech Authorship
Others
WOS Accession No
WOS:000882962300001
ESI Research Field
CHEMISTRY
Scopus EID
2-s2.0-85141997033
Data Source
Scopus
Citation statistics
Cited Times [WOS]:2
Document TypeJournal Article
Identifierhttp://kc.sustech.edu.cn/handle/2SGJ60CL/416490
DepartmentSouthern 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.
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.
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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