反应详情

To a mixture of 6-fluoro-3-(4-piperidinyl)-1H-indazole (438 mg, 2 mmol) and dry potassium carbonate (1.1 g, 6 mmol) in 30 ml methyl isobutyl ketone was added 3-bromo-1-propanol (276 mg, 2 mmol). The mixture was refluxed for 48 h, cooled, filtered and concentrated in vacuo. The crude product was purified by chromatography on silica gel 60 eluting with ethyl acetate:methanol (9:1, v/v). Concentration of the appropriate fractions afforded 300 mg (53%) of 3-[1-(1-hydroxyprop-3-yl)-4-piperidinyl]-6-fluoro-1 H-indazole as an oil.

1. temperatureThe mixture was refluxed for 48 h
2. temperaturecooled
3. filtrationfiltered
4. concentrationconcentrated in vacuo
5. customThe crude product was purified by chromatography on silica gel 60 eluting with ethyl acetate:methanol (9:1