Add time:08/05/2019         Source:sciencedirect.com

An approach to the synthesis (4-di- and -trifluoroalkyl-1-alkyl-1H-pyrazol-3-yl)methylamines – promising building blocks for drug discovery and medicinal chemistry is described. The key step of the reaction sequence is fluorination of the corresponding non-symmetric trisubstituted pyrazole derivatives bearing phtalimide moiety with diethylaminosulfur trifluoride or sulfur tetrafluoride. The title compounds are obtained in 5–6 steps from the commonly available materials and 35–36% overall yields.

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