三甲基硅基三氟溴甲烷对 2-吡啶酮、异喹啉酮和喹啉酮的化学选择性 - 和 - 二氟甲基化。
Chemoselective - and -Difluoromethylation of 2-Pyridones, Isoquinolinones, and Quinolinones with TMSCFBr.
机构信息
Loker Hydrocarbon Research Institute and Department of Chemistry, University of Southern California, Los Angeles, California 90089-1661, United States.
出版信息
Org Lett. 2021 Aug 20;23(16):6494-6498. doi: 10.1021/acs.orglett.1c02305. Epub 2021 Aug 3.
An operationally simple protocol for direct - and -difluoromethylation of 2-pyridones, quinolinones, and isoquinolinones using commercially available TMSCFBr is disclosed. The chemoselectivity is modulated by simple variations in temperature, solvent, and strength of the base. Diverse, synthetically relevant functional groups are tolerated, including functional groups that have reported reactivity with TMSCFBr. Gram-scale reactions to prepare both - and -difluoromethyl compounds are included.
本文公开了一种使用市售的 TMSCFBr 对 2-吡啶酮、喹啉酮和异喹啉酮进行直接 - 和 - 二氟甲基化的操作简单的方法。通过简单改变温度、溶剂和碱的强度来调节化学选择性。包括与 TMSCFBr 报道的反应性的官能团在内的各种合成相关的官能团都可以被容忍。包括制备 - 和 - 二氟甲基化合物的克级反应。
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