反应详情

A mixture of 7-benzyloxy-4-chloro-6-methoxyquinoline hydrochloride (300 mg, 0.89 mmol), (prepared as described for the starting material in Example 3), and 4-chloro-2-fluoroaniline (160 mg, 1.1 mmol) was heated at reflux in cyclohexane (20 ml) for 24 hours. The solvent was removed by evaporation and the residue was triturated with ether. The solid crude product was collected by filtration and purified by column chromatography eluting with methylene chloride/methanol (100/0 increasing to 95/5) to give 7-benzyloxy-4-(4-chloro-2-fluoroanilino)-6-methoxyquinoline hydrochloride (83 mg, 21%).

1. custom(prepared
2. temperaturewas heated
3. customThe solvent was removed by evaporation
4. customthe residue was triturated with ether
5. filtrationThe solid crude product was collected by filtration
6. custompurified by column chromatography
7. washeluting with methylene chloride/methanol (100/0 increasing to 95/5)