反应详情

1-phenyl-3-trifluoromethyl-1H-pyrazole-4-carboxylic acid (150 mg, 0.57 mmol), EDCI (280.6 mg, 1.5 mmol), methyl 3-aminopropionate (163.5 mg, 1.17 mmol), HOBt (118.7 mg, 0.8 mmol) and ethyldiisopropylamine (265.5 mg, 2.1 mmol) dissolved in dichloromethane (15 mL) were stirred for 24 hours. The reaction mixture was diluted with aqueous NaHCO3 and extracted with dichloromethane. The extract was washed with brine and dried with anhydrous sodium sulfate and concentrated under vacuum. The residue was purified by silica gel column chromatography to obtain the desired compound (181 mg, 91%) as a white solid.

1. extractionextracted with dichloromethane
2. washThe extract was washed with brine
3. dry with materialdried with anhydrous sodium sulfate
4. concentrationconcentrated under vacuum
5. customThe residue was purified by silica gel column chromatography