反应详情

温度

100 °C

Under an argon atmosphere, a suspension of methyl 5-bromo-1-(phenylsulfonyl)-1H-pyrrole-3-carboxylate (2.11 g), cyclopropylboronic acid (683 mg), palladium(II) acetate (69 mg), tricyclohexylphosphine (174 mg) and tripotassium phosphate (4.55 g) in toluene (27 mL)-water (1.3 mL) was stirred at 100° C. for 4 hr. After cooling, the reaction mixture was diluted with water (50 mL), and the mixture was extracted with ethyl acetate. The extract was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluent: hexane-ethyl acetate=19:1→8:2) to give the title compound as a yellow oil (yield 406 mg, 22%).

1. temperatureAfter cooling
2. extractionthe mixture was extracted with ethyl acetate
3. washThe extract was washed with saturated brine
4. dry with materialdried over anhydrous magnesium sulfate
5. concentrationconcentrated under reduced pressure
6. customThe residue was purified by silica gel column chromatography (eluent: hexane-ethyl acetate=19:1→8:2)