Tung Truong Thanh, Christensen Søren Brøgger, Nielsen John
Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark.
Chemistry. 2017 Dec 22;23(72):18125-18128. doi: 10.1002/chem.201704261. Epub 2017 Oct 11.
A technically simple procedure for direct C-H difluoromethylation of heteroaromatic compounds using off-the-shelf difluoroacetic acid as the difluoromethylating reagent has been developed. Mono-difluoromethylation versus bis-difluoromethylation is controlled as the result of the reaction temperature. The reactions described here enable access to the late-stage C-H mono- and bis-difluoromethylation for preparation of tool compounds for chemical biology and provide access to this hitherto untapped substituent for drug discovery.
已经开发出一种技术上简单的程序，使用市售的二氟乙酸作为二氟甲基化试剂，对杂环芳族化合物进行直接C-H二氟甲基化。单二氟甲基化与双二氟甲基化可通过反应温度来控制。本文所述的反应能够实现后期C-H单二氟甲基化和双二氟甲基化，以制备化学生物学工具化合物，并为药物发现提供这种迄今未开发的取代基。
