Difluoroacetic Acid as a New Reagent for Direct C-H Difluoromethylation of Heteroaromatic Compounds

被引：84
|
作者：
Truong Thanh Tung [1 ]
Christensen, Soren Brogger [1 ]
Nielsen, John [1 ]
机构：
[1] Univ Copenhagen, Dept Drug Design & Pharmacol, Univ Pk 2, DK-2100 Copenhagen, Denmark
来源：
CHEMISTRY-A EUROPEAN JOURNAL | 2017年 / 23卷 / 72期
关键词：
difluoroacetic acid; difluoromethylation; drug discovery; fluorine; radicals; COPPER-MEDIATED DIFLUOROMETHYLATION; CROSS-COUPLING REACTION; CATALYZED DIFLUOROMETHYLATION; (DIFLUOROMETHYL)ZINC REAGENT; DECARBOXYLATIVE FLUORINATION; MEDICINAL CHEMISTRY; ARYLBORONIC ACIDS; ARYL HALIDES; DRUG DESIGN; IODIDES;
D O I：
10.1002/chem.201704261
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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.
引用
收藏
页码：18125 / 18128
页数：4
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