反应详情

To a solution of the 5-(4-piperidinyloxy)-1H-indazole (100 mg, 0.460 mmol) obtained in Example 42 in N,N-dimethylformamide (3 ml) were added (2-bromoethyl)methyl ether (76.8 mg, 0.552 mmol) and potassium carbonate (159 mg, 1.15 mmol), and the resulting mixture was stirred overnight at room temperature. Then, the reaction solution was cooled to 0° C. and a saturated aqueous sodium hydrogencarbonate solution was added thereto, followed by extraction with ethyl acetate. The organic layer was washed with a saturated aqueous sodium chloride solution and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure and the resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol) to obtain 5-{[1-(2-methoxyethyl)piperidin-4-yl]oxy}-1H-indazole (52 mg, 41%).

1. temperatureThen, the reaction solution was cooled to 0° C.
2. extractionfollowed by extraction with ethyl acetate
3. washThe organic layer was washed with a saturated aqueous sodium chloride solution
4. dry with materialdried over anhydrous sodium sulfate
5. distillationThe solvent was distilled off under reduced pressure
6. customthe resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol)