反应详情

To a solution of 6-(5-{1-[4-(cyclopropylsulfonyl)phenyl]-2-(tetrahydro-2H-pyran-4-yl)ethyl}-1H-pyrrol-2-yl)pyridin-3-ol (0.052 g) in acetone (5 mL) were added chloroacetone (0.01 mL), potassium carbonate (18 mg) and potassium iodide (2 mg), and the mixture was heated under reflux for 11 hr. A saturated aqueous ammonium chloride solution was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The extract was washed successively with water and saturated brine, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate:hexane=20:80-100:0, volume ratio) to give the title compound (0.038 g, yield 64%) as a colorless amorphous solid. MS: 509 (MH+).

1. temperaturethe mixture was heated
2. temperatureunder reflux for 11 hr
3. extractionthe mixture was extracted with ethyl acetate
4. washThe extract was washed successively with water and saturated brine
5. dry with materialdried over anhydrous magnesium sulfate
6. concentrationconcentrated under reduced pressure
7. customThe residue was purified by silica gel column chromatography (ethyl acetate:hexane=20:80-100:0, volume ratio)