反应详情

2M Aqueous sodium hydroxide solution (453 μl, 0.9 mmol) was added to a suspension of 4-(2-fluoro-5-methoxycarbonyloxy-4-methylanilino)-7-(3-morpholinopropionamido)quinazoline (219 mg, 0.45 mmol) in methanol (6 ml) and the mixture stirred for 1 hour. The reaction mixture was diluted with water and then adjusted to pH6 with 2M hydrochloric acid. The resulting precipitate was collected by filtration, washed with water and ethanol, and dried. The solid was dissolved in methylene chloride/methanol and a 5M solution of hydrogen chloride in isopropanol (0.3 ml) added. The volatiles were removed by evaporation, the resulting solid was washed with ether, and dried under vacuum to give 4-(2-fluoro-5-hydroxy-4-methylanilino)-7-(3-morpholinopropionamido)quinazoline (1-86 mg, 80%) as a yellow solid.

1. filtrationThe resulting precipitate was collected by filtration
2. washwashed with water and ethanol
3. customdried
4. dissolutionThe solid was dissolved in methylene chloride/methanol
5. additiona 5M solution of hydrogen chloride in isopropanol (0.3 ml) added
6. customThe volatiles were removed by evaporation
7. washthe resulting solid was washed with ether
8. customdried under vacuum