反应详情

4-Morpholinylcarbonyl chloride (35 μl, 0.3 mmol) was added dropwise to a ice-cooled mixture of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-[(piperidin-4-yl)oxy]quinazoline (120 mg, 0.3 mmol) and diisopropylethylamine (63 μl, 0.36 mmol) in dichloromethane (5 ml). At the end of the addition, the mixture was stirred at room temperature for 18 hours. The mixture was diluted with dichloromethane, washed with water and brine and dried over magnesium sulfate. After evaporation of the solvents under vacuum, the residue was purified by chromatography on silica gel (eluant: 1% to 2% 7N methanolic ammonia in dichloromethane) to give the title compound as a white solid (100 mg, 64%).

1. temperaturecooled
2. additionAt the end of the addition
3. washwashed with water and brine
4. dry with materialdried over magnesium sulfate
5. customAfter evaporation of the solvents under vacuum
6. customthe residue was purified by chromatography on silica gel (eluant: 1% to 2% 7N methanolic ammonia in dichloromethane)