反应详情

5-[4-(Methylsulfonyl)phenoxy]-7-(tetrahydro-2H-pyran-4-ylmethoxy)-1H-indole-2-carboxamide (250 mg) was dissolved in N,N-dimethylformamide (5 mL), cyanuric chloride (311 mg) was added under ice-cooling, and the mixture was stirred for 1 hr. Water was added to the reaction solution, and the mixture was subjected to extraction with ethyl acetate. The organic layer was washed with saturated brine, dried over magnesium sulfate, filtered, and concentrated under reduced pressure. The obtained crude product was subjected to silica gel column chromatography (ethyl acetate:hexane=10:90-60:40, volume ratio) to give the title compound (240 mg, yield 100%) as a white solid. MS 445 (MH+).

1. temperaturecooling
2. extractionthe mixture was subjected to extraction with ethyl acetate
3. washThe organic layer was washed with saturated brine
4. dry with materialdried over magnesium sulfate
5. filtrationfiltered
6. concentrationconcentrated under reduced pressure
7. customThe obtained crude product