Journal of Fluorine Chemistry p. 72 - 81 (2018)
Update date:2022-08-03
Topics:
Nemytova
Shchegol'kov
Burgart, Ya.V.
Slepukhin
Borisevich
Khursan
Saloutin
The approaches for regiocontrolled N-, O- and C-methylation of 1-phenyl-3-polyfluoroalkyl-1H-pyrazol-5-ols have been developed. The chemoselective N-methylation proved to be an efficient method for the synthesis of polyfluorinated antipyrine analogs. In addition, we reinvestigated the structure of 3-polyfluoroalkyl-1-phenylpyrazol-5-ols by the X-Ray analysis. The quantum-chemical calculations were used for an explanation of methylation processes. The preliminary biological testing revealed a significant analgesic activity of trifluoromethyl-containing antipyrine.
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