反应详情

To a solution of 4-(4-amino-2-fluorophenoxy)-3-chloro-N-(diphenylmethylene)pyridin-2-amine (836 mg, 2.0 mmol) and 5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid (490 mg, 2.0 mmol) in DMF (10 mL) at room temperature were added HATU (913 mg, 2.4 mmol) and DIPEA (1.05 ml, 6.0 mmol). The reaction mixture was stirred at room temperature for 3 h prior to being quenched by the addition of cold water (50 mL). The solid that formed was collected by filtration, and washed with water and ether. The solid was dissolved in DCM and purified by flash column chromatography (SiO2, DCM to 10% MeOH in DCM) to give the desired product (987 mg, 78%) as a light yellow solid. MS (ESI+) m/z 633 (M+H)+.

1. customto being quenched by the addition of cold water (50 mL)
2. customThe solid that formed
3. filtrationwas collected by filtration
4. washwashed with water and ether
5. dissolutionThe solid was dissolved in DCM
6. custompurified by flash column chromatography (SiO2, DCM to 10% MeOH in DCM)