反应详情

2.15 g (12.8 mmol) of ethyl 2-fluorobenzoate and 1.9 g (14 mmol) of potassium carbonate are successively added to a solution of 4 g (12.8 mmol) of tert-butyl(4′-hydroxybiphenyl-3-ylmethyl)methylcarbamate in 45 ml of dimethylacetamide. The reaction medium is refluxed for 48 hours, cooled, diluted with water and extracted with ethyl acetate. The organic phase is dried over sodium sulfate, filtered and concentrated under vacuum. The residue obtained is purified by chromatography on a column of silica eluted with an 80/20 heptane/ethyl acetate mixture. 3.1 g of ethyl 2-{3′-[(tert-butoxycarbonylmethylamino)methyl]biphenyl-4-yloxy}benzoate are obtained in the form of a colorless oil, in a yield of 53%.

1. temperatureThe reaction medium is refluxed for 48 hours
2. temperaturecooled
3. extractionextracted with ethyl acetate
4. dry with materialThe organic phase is dried over sodium sulfate
5. filtrationfiltered
6. concentrationconcentrated under vacuum
7. customThe residue obtained
8. customis purified by chromatography on a column of silica
9. washeluted with an 80/20 heptane/ethyl acetate mixture