反应详情

温度

95 °C

A suspension of 7-benzyloxy-4-chloro-6-methoxyquinazoline free base (10 g, 33.2 mmol), 4-fluoro-5-hydroxy-2-methylindole (5.9 g, 35.7 mmol), (prepared as described for the starting material in Example 1), and potassium carbonate (9.2 g, 66.6 mmol) in NMP (100 ml) was stirred at 95° C. for 1 hour. After cooling, the mixture was partitioned between ethyl acetate and aqueous sodium hydrogen carbonate. The organic layer was separated, washed with brine and dried over magnesium sulphate and evaporated under vacuum. The residue was triturated under acetonitrile and the suspension was cooled. The precipitate was filtered and dried under vacuum to give 7-benzyloxy-4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxyquinazoline (8.2 g, 57%).

1. custom(prepared
2. temperatureAfter cooling
3. customthe mixture was partitioned between ethyl acetate and aqueous sodium hydrogen carbonate
4. customThe organic layer was separated
5. washwashed with brine
6. dry with materialdried over magnesium sulphate
7. customevaporated under vacuum
8. customThe residue was triturated under acetonitrile
9. temperaturethe suspension was cooled
10. filtrationThe precipitate was filtered
11. customdried under vacuum