在烯基C=C键上引入CF3基团。最近的进展

IF 1.7 4区 化学 Q3 CHEMISTRY, INORGANIC & NUCLEAR
Karolina Paszek, Henryk Koroniak, Katarzyna Koroniak–Szejn
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引用次数: 0

摘要

近年来,含氟药物引起了人们极大的兴趣。药物分子中氟基团的数量和类型决定了药物的生物学效应。通过研究肽结构的化学修饰来提高生物活性、体内稳定性或生物利用度也受到了很大的关注。最常被研究的含氟官能团是三氟甲基,它也以C(sp2) -CF3键的形式出现。三氟甲基烷基结构有助于肽保持其原始的β-转结构,有效地模仿天然肽键,使其具有同位体的功能。因此,开发合成三氟甲基烯烃的方法越来越受欢迎,因为这些产品有可能成为生物活性分子的组成部分。综述了利用三氟化试剂通过过渡金属介导和无过渡金属的三氟甲基化反应制备含三氟甲基烯烃化合物的各种方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Introducing CF3 group at alkenyl C=C bond. Recent developments

Introducing CF3 group at alkenyl C=C bond. Recent developments
Recently, significant interest has been developed in pharmaceuticals containing fluorine The biological effects depend on the number and type of fluorine groups in the drug molecule. Much attention has been also paid to improve biological activity, in vivo stability, or bioavailability by studying the chemical modification of peptide structure. The most frequently studied fluorine-containing functional group is the trifluoromethyl group, which also occurs as a C(sp2)–CF3 bond. The trifluoromethyl alkyl group structure helps the peptide maintain its original β-turn structure, effectively mimicking the natural peptide bond, which allows it to function as its isostere. Therefore, the development of methods for synthesizing the trifluoromethylalkene group is becoming increasingly popular due to the potential of the products as building blocks of bioactive molecules. This review describes various methods for the preparation of the compounds with a trifluoromethylalkene group using trifluorinating reagents via the transition metal-mediated and the transition metal-free trifluoromethylation reactions.
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来源期刊
Journal of Fluorine Chemistry
Journal of Fluorine Chemistry 化学-无机化学与核化学
CiteScore
3.80
自引率
10.50%
发文量
99
审稿时长
33 days
期刊介绍: The Journal of Fluorine Chemistry contains reviews, original papers and short communications. The journal covers all aspects of pure and applied research on the chemistry as well as on the applications of fluorine, and of compounds or materials where fluorine exercises significant effects. This can include all chemistry research areas (inorganic, organic, organometallic, macromolecular and physical chemistry) but also includes papers on biological/biochemical related aspects of Fluorine chemistry as well as medicinal, agrochemical and pharmacological research. The Journal of Fluorine Chemistry also publishes environmental and industrial papers dealing with aspects of Fluorine chemistry on energy and material sciences. Preparative and physico-chemical investigations as well as theoretical, structural and mechanistic aspects are covered. The Journal, however, does not accept work of purely routine nature. For reviews and special issues on particular topics of fluorine chemistry or from selected symposia, please contact the Regional Editors for further details.
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