期刊
CHEMICAL COMMUNICATIONS
卷 55, 期 91, 页码 13638-13648出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9cc07677h
关键词
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资金
- NSFC [21725203, 21901074]
- Ministry of Education (PCSIRT)
- Fundamental Research Funds for the Central Universities
- Zijiang Scholar Program of East China Normal University
The judicious incorporation of a fluoroalkyl moiety often brings about beneficial effects on the properties of bioactive molecules. Consequently, efficient methods for selective fluoroalkylation are much sought after in drug discovery. Despite significant achievements in trifluoromethylation, selective mono- and difluoroalkylation is still undeveloped. Catalytic functionalization of fluorinated silyl enol ethers (FSEEs) emerges as a fruitful approach for the diversity-oriented synthesis of value-added alpha-mono or difluoroalkylated ketones. In this feature article, we detail our efforts in developing catalytic selective mono- and difluoroalkylation reactions using FSEEs. Specifically, we highlight our findings such as activating FSEEs by amines for catalytic enantioselective synthesis, taking advantage of the often observed high activity of FSEEs over the non-fluorinated analogues for reaction development, and the influence of C-FMIDLINE HORIZONTAL ELLIPSISH-X interactions on reactivity and selectivity.
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