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Solid-State Radical C-H Trifluoromethylation Reactions Using Ball Milling and Piezoelectric Materials.
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2020-09-11 , DOI: 10.1002/anie.202009844
Yadong Pang 1 , Joo Won Lee 2 , Koji Kubota 1, 2 , Hajime Ito 1, 2
Affiliation  

The application of piezoelectricity for the generation of trifluoromethyl (CF3) radicals is reported together with the development of a method for the mechanochemical C−H trifluoromethylation of aromatic compounds. As compared to conventional solution‐based approaches, this mechanoredox C−H trifluoromethylation enables cleaner and more sustainable access to a wide range of trifluoromethylated N‐heterocycles and peptides, which are important structural motifs in modern drug discovery. This study thus represents an important milestone for future applications of mechanoredox systems to medicinal and pharmaceutical science.

中文翻译:

使用球磨和压电材料的固态自由基CH三氟甲基化反应。

伴随着压电技术在产生三氟甲基(CF 3)自由基方面的应用,以及对芳香族化合物CHH三氟甲基化的机械化学方法的开发,已有报道。与传统的基于解决方案的方法相比,这种机械的CH三氟甲基化可以更清洁,更可持续地访问各种三氟甲基化的N-杂环和肽,它们是现代药物发现中的重要结构图案。因此,这项研究代表了机械氧化还原系统在医学和药学领域未来应用的重要里程碑。
更新日期:2020-09-11
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