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含三氟甲基杂环化合物——三氟甲基砌块合成的最新进展

Recent advances in the synthesis of trifluoromethyl-containing heterocyclic compounds trifluoromethyl building blocks.

作者信息

Liu Yaopeng, Tian Qingyu, Ge Jin, Wu Xi, Li Zhenghao, Cheng Guolin

机构信息

Xiamen Key Laboratory of Optoelectronic Materials and Advanced Manufacturing, College of Materials Science and Engineering, Huaqiao University, Xiamen, 361021, China.

Key Lab of Fluorine and Silicon for Energy Materials and Chemistry of Ministry of Education, Jiangxi Normal University, Nanchang, 330022, China.

出版信息

Org Biomol Chem. 2024 Aug 7;22(31):6246-6276. doi: 10.1039/d4ob00877d.

DOI:10.1039/d4ob00877d
PMID:39041070
Abstract

Trifluoromethylated heterocyclic compounds have played an increasingly significant role in pharmaceuticals, agrochemicals, and materials. This is because the introduction of trifluoromethyl could enhance the lipophilicity, metabolic stability, and pharmacokinetic properties of heterocyclic drug molecules. Therefore, the synthesis of trifluoromethylated heterocyclics has become a major subject of research. The construction of trifluoromethylated heterocyclics the annulation of trifluoromethyl building blocks with suitable partners has been proved to be a powerful strategy. In this review, we systematically summarize and discuss recent advances in the preparation of trifluoromethyl-containing heterocyclics trifluoromethyl building block strategies over the period from 2019 to the present.

摘要

三氟甲基化杂环化合物在药物、农用化学品和材料领域发挥着越来越重要的作用。这是因为引入三氟甲基可以增强杂环药物分子的亲脂性、代谢稳定性和药代动力学性质。因此,三氟甲基化杂环化合物的合成已成为一个主要的研究课题。三氟甲基化杂环化合物的构建——将三氟甲基砌块与合适的底物进行环化反应——已被证明是一种有效的策略。在本综述中,我们系统地总结并讨论了自2019年至今期间,通过三氟甲基砌块策略制备含三氟甲基杂环化合物的最新进展。

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