反应详情

To a mixture of 5-(5-chloro-2-hydroxyphenyl)indolin-2-one (0.132 g, 0.51 mmol) and potassium carbonate (0.105 g, 0.76 mmol) in dimethylsulfoxide (3 mL) was added N-(2,4-dimethoxybenzyl)-2,4,5-trifluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide (0.239 g, 0.54 mmol). The reaction mixture was degassed with nitrogen for 10 minutes and stirred for 16 h at ambient temperature. The reaction mixture was partitioned between ethyl acetate (50 mL) and water (5 mL). The organic phase was washed with water (2 5 mL) and brine (2 5 mL), dried over anhydrous sodium sulphate, filtered and concentrated in vacuo. The residue was purified by column chromatography, eluting with a 10-50% gradient of ethyl acetate in hexanes to afford 4-(4-chloro-2-(2-oxoindolin-5-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide as a colorless foam that was carried forward without further purification.

1. customThe reaction mixture was degassed with nitrogen for 10 minutes
2. customThe reaction mixture was partitioned between ethyl acetate (50 mL) and water (5 mL)
3. washThe organic phase was washed with water (2 5 mL) and brine (2 5 mL)
4. dry with materialdried over anhydrous sodium sulphate
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. customThe residue was purified by column chromatography
8. washeluting with a 10-50% gradient of ethyl acetate in hexanes