反应详情

To a solution of N-(4-((2-aminopyridin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (200 mg, 0.48 mmol) in DCM (5 mL) was added triethylamine (1 mL), followed by adding cyclopropanecarbonyl chloride (104.5 mg, 0.96 mmol) at 0° C. The reaction mixture was warmed to rt and stirred for 3 hours, then quenched with water (10 mL). The separated organic layer was added saturated aq. Na2CO3 (10 mL) and EtOH (30 mL). The mixture was stirred at rt for 30 minutes and concentrated in vacuo. The residue was purified by a silica gel column chromatography (DCM/MeOH (v/v)=80/1) to give the title compound as a white solid (130 mg, 56%).

1. customquenched with water (10 mL)
2. additionThe separated organic layer was added saturated aq. Na2CO3 (10 mL) and EtOH (30 mL)
3. stirringThe mixture was stirred at rt for 30 minutes
4. concentrationconcentrated in vacuo
5. customThe residue was purified by a silica gel column chromatography (DCM/MeOH (v/v)=80/1)