反应详情

Acetic acid 1-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-6-ylcarbamoyl)-ethyl ester 9a (2.035 g, 6.9 mmol) was dissolved in 20 ml of methanol under stirring, added with sodium hydroxide solution (20 ml, 0.7 mol/L) (20 ml) to the solution and stirred for 4 hours at room temperature. After thin lay chromatography showed the disappearance of starting materials, the reaction mixture was neutralized with hydrochloride acid (1 mol/L) and concentrated under reduced pressure. The residue was purified by silica gel column chromatography and dried to obtain N-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-6-yl)-2-hydroxy-2-methyl-propionamide 9b (900 mg, yield 59.2%) as a white solid.

1. stirringstirred for 4 hours at room temperature
2. concentrationconcentrated under reduced pressure
3. customThe residue was purified by silica gel column chromatography
4. customdried