反应详情

温度

50 °C

A mixture of 4-(5-benzyloxy-2-fluoro4-methylanilino)-7-hydroxy-6-methoxyquinazoline (440 mg, 1 mmol), 2-bromoethanol (77 ml, 1 mmol) and potassium carbonate (150 mg, 1.1 mmol) in DMF (5 ml) was heated at 50° C. for 1 hour, further 2-bromoethanol (42 ml, 0.6 mmol) and potassium carbonate (150 mg, 1.1 mmol) was added and the mixture was maintained at 50° C. for 2 hours. The reaction mixture was diluted with water, neutralised with 2M hydrochloric acid and extracted with ethyl acetate. The extracts were dried (MgSO4), the solvent removed by evaporation and the residue triturated with ether and hexane to give 4-(5-benzyloxy-2-fluoro-4-methylanilino)-7-(2-hydroxyethoxy)-6-methoxyquinazoline (200 mg, 41%).

1. temperaturethe mixture was maintained at 50° C. for 2 hours
2. extractionextracted with ethyl acetate
3. dry with materialThe extracts were dried (MgSO4)
4. customthe solvent removed by evaporation
5. customthe residue triturated with ether and hexane