Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 23, Issue 72, Pages 18125-18128Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201704261
Keywords
difluoroacetic acid; difluoromethylation; drug discovery; fluorine; radicals
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Funding
- University of Copenhagen Excellency Program for Interdisciplinary Excellence [UC2016]
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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.
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