反应详情

温度

90 °C

4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-7-hydroxy-6-methoxyquinazoline (250 mg, 0.74 mmol), (prepared as described for the starting material in this example hereinbefore), and potassium carbonate (112 mg, 0.81 mmol) were stirred together in N-methylpyrrolidinone (3 ml). 1-Acetyl-4-(3-chloropropoxy)piperazine (166 mg, 0.81 mmol) in N-methylpyrrolidinone (1 ml) was added and the mixture heated at 90° C. for 3 hours. The mixture was cooled, filtered and concentrated under reduced pressure. The residue was purified by column chromatography eluting with methylene chloride/methanol (saturated with ammonia) (97/3) to give 7-[3-(4-acetylpiperazin-1-yl)propoxy]-4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinazoline (268 mg, 71%) as a white solid.

1. temperatureThe mixture was cooled
2. filtrationfiltered
3. concentrationconcentrated under reduced pressure
4. customThe residue was purified by column chromatography
5. washeluting with methylene chloride/methanol (saturated with ammonia) (97/3)