反应详情

To a solution of 2-[4,6-bis(4-fluorophenyl)-5-(4-pyridyl)pyrazolo[3,4-b]pyridin-2-yl]acetic acid (0.05 g, 0.1 mmol, obtained in example 44) in DMF (1 mL), N,N′-dicyclohexylcarbodiimide (0.02 g, 0.1 mmol) and 1-hydroxybenzotriazole (0.02 g, 0.1 mmol) were added under argon atmosphere. The mixture was stirred for 15 min and morpholine (0.01 g, 0.1 mmol) was added. This was stirred at room temperature for 2 days. EtOAc was added and the mixture was filtered. The filtrate was washed with saturated NaHCO3. The organic phase was dried over Na2SO4 and concentrated to dryness. The crude product obtained was purified by chromatography on silica gel using EtOAc-MeOH mixtures of increasing polarity as eluent, to afford 18 mg of title compound (yield: 35%).

1. stirringThis was stirred at room temperature for 2 days
2. filtrationthe mixture was filtered
3. washThe filtrate was washed with saturated NaHCO3
4. dry with materialThe organic phase was dried over Na2SO4
5. concentrationconcentrated to dryness
6. customThe crude product obtained
7. customwas purified by chromatography on silica gel
8. temperatureof increasing polarity as eluent