反应详情

Palladium acetate (62 mg) and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (170 mg) were dissolved in toluene (16 ml) to prepare a solution which was then stirred at room temperature for 5 min. 4-Chloro-6-methoxy-quinolin-7-yl trifluoro-methanesulfonate (400 mg) and 2-morpholin-4-yl-ethylamine (1.12 ml) were added thereto, and the mixture was further stirred at room temperature for 5 min. Cesium carbonate (1.97 g) was added to the reaction solution, and the mixture was stirred at 90° C. overnight. Water was added to the reaction solution, and the mixture was extracted with chloroform. The chloroform layer was then washed with water and was dried over anhydrous sodium sulfate. The solvent was removed by distillation under the reduced pressure, and the residue was purified by thin layer chromatography using methanol chloroform to give (4-chloro-6-methoxy-quinolin-7-yl)-(2-morpholin-4-yl-ethyl)-amine (53 mg, yield 14%).

1. customto prepare a solution which
2. stirringthe mixture was further stirred at room temperature for 5 min
3. stirringthe mixture was stirred at 90° C. overnight
4. extractionthe mixture was extracted with chloroform
5. washThe chloroform layer was then washed with water
6. dry with materialwas dried over anhydrous sodium sulfate
7. customThe solvent was removed by distillation under the reduced pressure
8. customthe residue was purified by thin layer chromatography