反应详情

A solution of 7-benzyloxy-4-(4-chloro-2,6-difluoroanilino)-6-methoxyquinazoline (200 mg, 0.47 mmol) in TFA (3 ml) was stirred at 80° C. for 3 hours. After cooling, the volatiles were removed under vacuum and the residue was dissolved in water containing 5% methanol. The pH was adjusted to 8 with sodium hydrogen carbonate and the solid was collected by filtration and washed with water. The solid was solubilised in a mixture of ethyl acetate/methanol/methylene chloride (47/6/47). The volatiles were removed under vacuum to give 4-(4-chloro-2,6-difluoroanilino)-7-hydroxy-6-methoxyquinazoline (126 mg, 80%).

1. temperatureAfter cooling
2. customthe volatiles were removed under vacuum
3. dissolutionthe residue was dissolved in water containing 5% methanol
4. filtrationthe solid was collected by filtration
5. washwashed with water
6. additionThe solid was solubilised in a mixture of ethyl acetate/methanol/methylene chloride (47/6/47)
7. customThe volatiles were removed under vacuum