反应详情

温度

50 °C

To a solution of 7-hydroxy-4-(1H-indol-5-yloxy)-6-methoxyquinazoline (1 g, 3.2 mmol), (prepared as described for the starting material in Example 107), in DMF (50 ml) was added powdered potassium carbonate (1.32 g, 9.6 mmol) and 1,3-dibromopropane (6.43 g, 32 mmol). The reaction was heated at 50° C. for 2 hours. The inorganic material was filtered off and then the DMF removed. The residue was partitioned between methylene chloride/water. The organics were separated, dried over MgSO4, filtered, evaporated in vacuo and purified by flash chromatography eluting from methylene chloride to 5% methanol/95% methylene chloride. The product was concentrated in vacuo, triturated with ether and the resulting solid filtered to give 7-(3-bromopropoxy)-4-(1H-indol-5-yloxy)-6-methoxyquinazoline (900 mg, 66%) as a white solid.

1. filtrationThe inorganic material was filtered off
2. customthe DMF removed
3. customThe residue was partitioned between methylene chloride/water
4. customThe organics were separated
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. customevaporated in vacuo
8. custompurified by flash chromatography
9. washeluting from methylene chloride to 5% methanol/95% methylene chloride
10. concentrationThe product was concentrated in vacuo
11. customtriturated with ether
12. filtrationthe resulting solid filtered