反应详情

10% palladium on carbon (82 mg) was added to a solution of 2-amino-N-(7-chloro-4-methoxy-quinolin-8-yl)-4-trifluoromethyl-benzenesulfonamide (Intermediate 195) (670 mg, 1.5 mmol) and ammonium formate (481 mg, 7.5 mmol) in 50% acetic acid (5 ml) and the reaction was heated under reflux for 30 min. After cooling the mixture was diluted with EtOAc (100 ml), washed sat sodium bicarbonate solution, dried (MgSO4) concentrated in vacuo. The crude residue was purified by column chromatography with DCM/MeOH (98:2) as the eluent to give the title compound (604 mg, 100%).

1. temperaturethe reaction was heated
2. temperatureunder reflux for 30 min
3. temperatureAfter cooling the mixture
4. washwashed
5. dry with materialdried (MgSO4)
6. concentrationconcentrated in vacuo
7. customThe crude residue was purified by column chromatography with DCM/MeOH (98:2) as the eluent