反应详情

温度

85 °C

4-Chloro-7-{2-[4-(2-fluoroethyl)piperazin-1-yl]ethoxy}-6-methoxyquinazoline (172 mg, 0.47 mmol) was dissolved in dimethylacetamide (5 ml). 5-Hydroxy-7-azaindole (69 mg, 0.51 mmol), (prepared as described for the starting material in Example 2), and potassium carbonate (71 mg, 0.51 mmol) were added and the mixture heated to 85° C. for 4 hours. The reaction mixture was cooled, filtered and concentrated. The resulting residue was purified by column chromatography eluting with methylene chloride/methanol (saturated with ammonia) (94/6). The fractions containing the expected product were evaporated under vacuum and the residue was suspended in acetone, filtered and dried under vacuum to give 4-(7-azaindol-5-yloxy)-7-(2-[4-(2-fluoroethyl)piperazin-1-yl]ethoxy)-6-methoxyquinazoline (123 mg, 56%).

1. additionwere added
2. temperatureThe reaction mixture was cooled
3. filtrationfiltered
4. concentrationconcentrated
5. customThe resulting residue was purified by column chromatography
6. washeluting with methylene chloride/methanol (saturated with ammonia) (94/6)
7. additionThe fractions containing the expected product
8. customwere evaporated under vacuum
9. filtrationfiltered
10. customdried under vacuum