反应详情

温度

70 °C

A mixture of 6-methoxy-4-[(3-methyl-1H-indol-5-yl)oxy]-7-[(piperidin-4-yl)methoxy]quinazoline (0.2 g), chloroacetone (0.046 ml), potassium carbonate (0.1 g) and DMF (6 ml) was stirred and heated to 70° C. for 1 hour. The mixture was cooled to ambient temperature, the precipitate was removed by filtration, the solvent was removed by evaporation under vacuum and the residue was purified by column chromatography on silica using increasingly polar solvent mixtures, starting with dichloromethane and ending dichloromethane/methanol (93/7). Evaporation of the solvents gave a foam which was triturated under ether/pentane (70/30) to give a solid which was collected by filtration and dried under vacuum to give 7-{[1-(acetylmethyl)piperidin-4-yl]methoxy}-6-methoxy-4-[(3-methyl-1H-indol-5-yl)oxy]quinazoline (0.074 g).

1. temperatureThe mixture was cooled to ambient temperature
2. customthe precipitate was removed by filtration
3. customthe solvent was removed by evaporation under vacuum
4. customthe residue was purified by column chromatography on silica using
5. temperatureincreasingly polar solvent mixtures
6. customEvaporation of the solvents
7. customgave a foam which
8. customwas triturated under ether/pentane (70/30)
9. customto give a solid which
10. filtrationwas collected by filtration
11. customdried under vacuum