反应详情

温度

85 °C

A mixture of 7-[3-(4-acetylpiperazin-1-yl)propoxy]-4-chloro-6-methoxyquinazoline (190 mg, 0.50 mmol), (prepared as described for the starting material in Example 4), 5-hydroxy-2-methylindole (81 mg, 0.55 mmol), (WO 00/47212, Example 48), and potassium carbonate (76 mg, 0.55 mmol) in DMA (6 ml) was stirred at 85° C. for 3 hours, allowed to cool to ambient temperature and the solvent evaporated under vacuum. The residue was purified by column chromatography eluting with methylene chloride/methanol (saturated with ammonia) (92/8) to give a white solid. This was triturated with a mixture of ether and acetone, filtered and dried to give 7-[3-(4-acetylpiperazin-1-yl)propoxy]-6-methoxy-4-[(2-methyl-1H-indol-5-yl)oxy]quinazoline (130 mg, 53%).

1. custom(prepared
2. temperatureto cool to ambient temperature
3. customthe solvent evaporated under vacuum
4. customThe residue was purified by column chromatography
5. washeluting with methylene chloride/methanol (saturated with ammonia) (92/8)
6. customto give a white solid
7. customThis was triturated with a mixture of ether and acetone
8. filtrationfiltered
9. customdried