反应详情

To a suspension of 3-(3-methylquinoxalin-2-yl)-1H-pyrazol-5-amine (5.00 g, 22.2 mmol) and ethyl hydrogen malonate (2.88 mL, 24.4 mmol) in pyridine (89 mL) was added N-ethyl-N′-(3-dimethylaminopropyl)carbodiimide hydrochloride (6.38 g, 33.3 mmol) at 0° C. and stirred for 30 min. The reaction mixture was stirred for 1 h at room temperature and then concentrated in vacuo. The residue was diluted with water (100 mL) and the resulting precipitate was collected and washed with water followed by diethyl ether to give ethyl 3-{[3-(3-methylquinoxalin-2-yl)-1H-pyrazol-5-yl]amino}-3-oxopropanoate. MS (APCI): m/z 340 (M+H).

1. stirringThe reaction mixture was stirred for 1 h at room temperature
2. concentrationconcentrated in vacuo
3. additionThe residue was diluted with water (100 mL)
4. customthe resulting precipitate was collected
5. washwashed with water