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Regioselective C−H Trifluoromethylation and Its Related Reactions of (Hetero)aromatic Compounds
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- Yoichiro Kuninobu
- Institute for Materials Chemistry and Engineering Interdisciplinary Engineering Sciences, Interdisciplinary Graduate School of Engineering Sciences Kyushu University 6-1 Kasugakoen Kasuga-shi Fukuoka 816-8580 Japan
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Description
<jats:title>Abstract</jats:title><jats:p>Fluorinated functional groups, including trifluoromethyl group, play important roles in the development of drugs, agrochemicals, and organic functional materials. Therefore, the development of highly effective and practical reactions to introduce fluorinated functional groups into (hetero)aromatic compounds is highly desirable. We have achieved several regioselective C−H trifluoromethylation and related reactions by electrophilic and nucleophilic activation of six‐membered heteroaromatic compounds and steric protection of aromatic compounds. These reactions proceed in good to excellent yields, even on a gram scale, with high functional group tolerance, and are applicable to the regioselective trifluoromethylation of drug molecules. In this personal account, the background of the introduction reactions of fluorinated functional groups, our reaction designs to achieve regioselective C−H trifluoromethylation and the related reactions of (hetero)aromatic compounds are explained.</jats:p>
Journal
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- The Chemical Record
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The Chemical Record 23 (9), 2023-03-10
Wiley
