With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13349-91-2,1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride,as a common compound, the synthetic route is as follows.
General procedure: To a stirred suspension of 5-chloro-2-[[5-methyl-3-(6-methyl-3-pyridyl)isoxazol-4- yl]methyl]pyridazin-3-one (building block A, 300 mg, 0.947 mmol) and (R)-3- hydroxypyrrolidine (0.14 mL, 1.73 mmol) in DMSO (0.5 mL) and acetonitrile (3 mL) was added potassium carbonate (393 mg, 2.84 mmol) Then the reaction mixture was stirred at 70 C for 18 h. After cooling to room temperature the reaction mixture was diluted with EtOAc (80 mL) was washed three times with water (10 mL) and brine (10 mL). The aqueous layers were back extracted twice with EtOAc (80 mL). The combined organic extracts were dried (Na2S04), filtered and concentrated in vacuo. Purification by flash chromatography (silica, gradient: 0% to 10% MeOH in CH2CI2) afforded the title compound (341 mg, 93 %) as an off-white foam. MS (ESI): 368.2 ([M+H]+).
13349-91-2, 13349-91-2 1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride 16312067, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CECERE, Giuseppe; GROEBKE ZBINDEN, Katrin; HERNANDEZ, Maria-Clemencia; KNUST, Henner; KOBLET, Andreas; OLIVARES MORALES, Andres Miguel; PATINY-ADAM, Angelique; PINARD, Emmanuel; RUNTZ-SCHMITT, Valerie; STEINER, Sandra; (328 pag.)WO2019/238633; (2019); A1;,
Piperazine – Wikipedia
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