反应详情

2.14 g (4.64 mmol) 5-{[(2-chloro-3-fluoro-4-methoxyphenyl)(2-trifluoromethyl-oxiranyl)methyl]amino}-7-fluoro-1H-quinolin-2-on obtained in example 3 are stirred with 2.57 g (7.9 mmol) Caesium carbonate in 37 ml methanol. After 3 days water is added and the aqueous phase is extracted with ethyl acetate. The combined organic phases are washed with brine and dried over sodium sulphate. After removal of the solvent flash chromatography on silica gel (methanol in dichloromethan 0 to 5%) yields 0.98 g of the title compound.

1. extractionthe aqueous phase is extracted with ethyl acetate
2. washThe combined organic phases are washed with brine
3. dry with materialdried over sodium sulphate
4. customAfter removal of the solvent flash chromatography on silica gel (methanol in dichloromethan 0 to 5%)