反应详情

To a solution of 4-(quinolin-4-yloxy)-benzene-1,2-diamine (Step B, 227 mg) in CH3CN (60 mL) was added over 5 min, a solution of 1-isothiocyanato-4-trifluoromethyl-benzene (183 mg) in CH3CN 10 mL). The mixture was stirred for 12 h at RT and EDC (260 mg) was added, followed by CH3CN (30 mL). The resulting mixture was heated at 80° C. for 2 h, then cooled to RT. The solvent was evaporated and the residue was dissolved in EtOAc and washed with water. The organic phase was dried, filtered and evaporated. The residue was purified by flash chromatography in EtOAc to give an orange-brown solid. MS (MH+)=420.9, MW: 420.18 Calc'd for: C23H15F3N4O.

1. temperatureThe resulting mixture was heated at 80° C. for 2 h
2. temperaturecooled to RT
3. customThe solvent was evaporated
4. dissolutionthe residue was dissolved in EtOAc
5. washwashed with water
6. customThe organic phase was dried
7. filtrationfiltered
8. customevaporated
9. customThe residue was purified by flash chromatography in EtOAc
10. customto give an orange-brown solid