反应详情

To a solution of N-(3,3-dimethyl-2-oxoindolin-6-yl)-3-fluoroisonicotinamide (example 72, 100 mg, 334 μmol) in DMF (1.67 ml) under an argon atmosphere was added methylsulfonylethene (35.5 mg, 31.6 μl, 334 μmol) and cesium carbonate (109 mg, 334 μmol). After 3 hours at room temperature the reaction mixture was poured into water and the aqueous phase was extracted with EtOAc. The combined organic layers were dried over Na2SO4 and the solvent was evaporated. The residue was purified by flash chromatography on silica gel using dichloromethane/methanol (with 10% ammonia) as eluent followed by preparative HPLC. The title compound was obtained as off-white solid (60 mg).

1. extractionthe aqueous phase was extracted with EtOAc
2. dry with materialThe combined organic layers were dried over Na2SO4
3. customthe solvent was evaporated
4. customThe residue was purified by flash chromatography on silica gel