These common heterocyclic compound, 52222-73-8, name is 4-(Trifluoromethyl)-1H-pyrazole, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. COA of Formula: C4H3F3N2
To a vial was added 3-iodo-N- isopropyl-l-[(4-methoxyphenyl)methyl]pyrazolo[4,3-c]pyridin-4-amine (100 mg, 0.237 mmol), 4-(trifiuoromethyl)-lH-pyrazole (30.6 mg, 0.225 mmol), copper(I) iodide (11.3 mg, 0.059 mmol), potassium carbonate (57.8 mg, 0.414 mmol). The vial was purged with nitrogen and toluene (0.47 mL, 4.45 mmol) and iras-N,N’-dimethylcyclohexane-l,2- diamine, (0.02 mL, 0.12 mmol) were added. The vial was sealed and heated to 110 C for 24 h. The reaction mixture was filtered through Celite, eluting with DCM and concentrated in vacuo. The crude residue was purified by column chromatography (0-20% EtOAc in DCM) to give the title compound which was used directly in the next step.
The synthetic route of 4-(Trifluoromethyl)-1H-pyrazole has been constantly updated, and we look forward to future research findings.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; CHAN, Bryan; ESTRADA, Anthony; SHORE, Daniel; SWEENEY, Zachary; WO2013/139882; (2013); A1;,
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