反应详情

温度

25 °C

To a solution of 2,6-dichloro-3-nitropyridine (0.67 g, 3.2 mmol) and DIEA (0.46 ml, 2.65 mmol) in EtOH (20 ml) was added 5-cyclopropyl-1H-pyrazol-3-amine (0.26 g, 2.12 mmol) solution in EtOH (5 ml) dropwise at 0° C. After addition, the reaction mixture was stirred at 25° C. for 24 hrs. The solvent was removed under reduced pressure and the resulted residue was purified by column chromatography (hexane-EtOAc=5:1) to give the title compound as a yellow solid (0.58 g, 98%). 1H NMR (400 MHz) δ□12.36 (s, 1H), 10.20 (s, 1H), 8.54 (d, J=8.4 Hz, 1H), 7.01 (d, J=8.4 Hz, 1H), 6.39 (d, J=1.6 Hz, 1H), 1.94 (m, 1H), 0.96 (m, 2H), 0.71 (m, 2H). MS: Calcd.: 279. Found: [M+H]+ 280.

1. additionAfter addition
2. customThe solvent was removed under reduced pressure
3. customthe resulted residue was purified by column chromatography (hexane-EtOAc=5:1)