反应详情

温度

130 °C

4-Chloro-7-methoxy-6-methoxycarbonylquinoline (1.4 g, 5.5 mmol) was dissolved in cyclohexanol (30 ml) and 4-chloro-2-fluoroaniline (0.786 g, 5.8 mmol) was added. The mixture was heated at 130° C. for 1 hour then at 160° C. for 3hours. The solvent was removed by evaporation and the residue was purified by flash chromatography eluting with methylene chloride/ethylacetate (100/0 increasing to 50/50). The solvent was removed by evaporation and the solid was triturated with ether/isohexanes. The solid was collected by filtration, washed with ether and dried under vacuum to give 4-(4-chloro-2-fluoroanilino)-7-methoxy-6-methoxycarbonylquinoline (570 mg, 28%).

1. customThe solvent was removed by evaporation
2. customthe residue was purified by flash chromatography
3. washeluting with methylene chloride/ethylacetate (100/0 increasing to 50/50)
4. customThe solvent was removed by evaporation
5. customthe solid was triturated with ether/isohexanes
6. filtrationThe solid was collected by filtration
7. washwashed with ether
8. customdried under vacuum