Adding a certain compound to certain chemical reactions, such as: 137890-05-2, name is 1-(1-Methyl-1H-pyrazol-5-yl)ethanone, belongs to pyrazoles-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 137890-05-2, COA of Formula: C6H8N2O
Under N2, a mixture of intermediate 1 lb (1 g) and 5-acetyl-l-methylpyrazole (168mgl.35 mmol) in THF (15 mL) was stirred at rt overnight. Then, NaBH(OAc)3 (718 mg;3.4 mmol) was added portion wise. The reaction mixture was stirred at room temperature for 72h, poured into cold water, basified with K2C03 powder and extracted with EtOAc. The organic layer was dried over MgSO4, filtered and evaporated to dryness. The residue was purified by chromatography over silica gel (irregular SiOH, 12g; mobile phase:gradient from 100% DCM, 0% MeOH to 95% DCM, 5% MeOH, 0.3% NH4OH). The fractions were collected and evaporated to dryness. The residue (300 mg) was purified asecond time by reverse phase chromatography (YMC-actus Triart Cl 8 1 Ojim30*150mm; mobile phase: gradient from 65% NH4HCO3 0.2% aq, 35% ACN to 25%NH4HCO3 0.2% aq, 75% ACN). The pure fractions were collected, evaporated to drynessyielding 104 mg of compound 224.
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Reference:
Patent; JANSSEN PHARMACEUTICA NV; ANGIBAUD, Patrick, Rene; PANDE, Vineet; HERKERT, Barbara; KROSKY, Daniel, Jason; QUEROLLE, Olivier, Alexis, Georges; PILATTE, Isabelle, Noelle, Constance; PATRICK, Aaron, Nathaniel; (250 pag.)WO2018/50686; (2018); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics