反应详情

温度

90 °C

To a degassed solution of 5-ethoxymethoxy-benzofuran boronic acid (4) (0.69 g, 2.63 mmol) in ethanol (17.5 mL), (5-bromo-6-nitro-pyridin-2-yl)-methyl-carbamic acid tert-butyl ester 12 (0.50 g, 1.51 mmol), Pd(PPh3)2Cl2 (0.14 g, 0.20 mmol) and Et3N (0.48 mL, 3.46 mmol) were added. The reaction mixture was stirred at 90° C. for 30 minutes. The reaction mixture was cooled to 0° C. and clear filtered. Volatiles were removed under reduced pressure. The residue was diluted with water and the mixture was extracted with ethyl acetate. The organic extract was washed with brine and concentrated under reduced pressure. The crude product was purified by flash column chromatography. Evaporation of solvent gave title compound 13 (58% yield).

1. temperatureThe reaction mixture was cooled to 0° C.
2. customVolatiles were removed under reduced pressure
3. additionThe residue was diluted with water
4. extractionthe mixture was extracted with ethyl acetate
5. extractionThe organic extract
6. washwas washed with brine
7. concentrationconcentrated under reduced pressure
8. customThe crude product was purified by flash column chromatography
9. customEvaporation of solvent