反应详情

To a solution of the 5-(piperidin-4-yloxy)-1H-indazole (31 mg, 0.143 mmol) obtained in Example 42 in N,N-dimethylformamide (1 ml) were added 2-bromoethanol (0.0121 ml, 0.171 mmol) and potassium carbonate (49 mg, 0.357 mmol). After 17 hours, 2-bromoethanol (0.0121 ml, 0.171 mmol) was further added thereto. After another 24 hours, the reaction mixture was filtered by the use of Celite and the filtrate was concentrated under reduced pressure. The resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol→chloroform/methanol/(1%-aqueous ammonia)) to obtain 2-[4-(1H-indazol-5-yloxy)piperidin-1-yl]ethanol (14 mg, 38%).

1. waitAfter another 24 hours
2. filtrationthe reaction mixture was filtered by the use of Celite
3. concentrationthe filtrate was concentrated under reduced pressure
4. customThe resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol→chloroform/methanol/(1%-aqueous ammonia))