The Journal of Organic Chemistry · 2018 · 37 citations · 59 references
Natural SciencesChemistryMedicinal ChemistryCatalysisGreen ChemistrySynthetic Medicinal ChemistryHeterocycle SynthesisSafer Chemical SynthesisHydrazone FormationPyrazine ChemistryPyrazole ChemistryPyrazole Synthesis
A novel and efficient protocol for the construction of trifluoroethyl pyrazolines has been developed by cascade cyclization/trifluoromethylation reaction of β,γ-unsaturated hydrazones. This strategy uses cheap and commercially available trichloroisocyanuric acid as promoter and TMSCF3 as the trifluoromethylating reagent, which make the trifluoromethylating process much cheaper. A wide range of substrates can be applied in this process to afford the trifluoroethyl pyrazolines in good yield.
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The Many Roles for Fluorine in Medicinal Chemistry
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