Difluoroacetic Acid as a New Reagent for Direct C-H Difluoromethylation of Heteroaromatic Compounds
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Difluoroacetic Acid as a New Reagent for Direct C-H Difluoromethylation of Heteroaromatic Compounds. / Thanh Tung, Truong; Christensen, Søren Brøgger; Nielsen, John.
In: Chemistry: A European Journal, Vol. 23, 11.10.2017, p. 18125-18128.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Difluoroacetic Acid as a New Reagent for Direct C-H Difluoromethylation of Heteroaromatic Compounds
AU - Thanh Tung, Truong
AU - Christensen, Søren Brøgger
AU - Nielsen, John
N1 - © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
PY - 2017/10/11
Y1 - 2017/10/11
N2 - 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.
AB - 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.
KW - Journal Article
U2 - 10.1002/chem.201704261
DO - 10.1002/chem.201704261
M3 - Journal article
C2 - 28945302
VL - 23
SP - 18125
EP - 18128
JO - Chemistry: A European Journal
JF - Chemistry: A European Journal
SN - 0947-6539
ER -
ID: 183760324