反应详情

温度

80 °C

A mixture of 7-{[1-(chloroacetyl)piperidin-4-yl]methoxy}-6-methoxy-4-[(3-methyl-1H-indol-5-yl)oxy]quinazoline (0.118 g), pyrrolidine (0.059 ml), potassium iodide (0.01 g) and DMF (3 ml) was stirred and heated to 80° C. for 40 minutes. The mixture was cooled to ambient temperature, 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 saturated with ammonia (3.5M) (94/6). 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 6-methoxy-4-[(3-methyl-1H-indol-5-yl)oxy]-7-{[1-(pyrrolidin-1-ylacetyl)piperidin-4-yl]methoxy}quinazoline (0.096 g).

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