反应详情

To N-{3-[(2-aminoimidazo[1,2-a]pyridin-6-yl)oxy]phenyl}-3-methylpyridine-2-carboxamide (150 mg, 0.417 mmol), tetrahydrofuran (10 mL) and aqueous sodium hydrogen carbonate solution (5 mL) was added cyclopropanesulfonyl chloride (348 μL, 2.48 mmol), and the mixture was stirred at room temperature for 61 hr. The reaction mixture was concentrated under reduced pressure, diluted with aqueous sodium hydrogen carbonate solution and extracted with ethyl acetate. The organic layer was washed with aqueous sodium hydrogen carbonate solution and saturated brine, dried over anhydrous magnesium sulfate and filtrated. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (0%→70% ethyl acetate-hexane) to give the title compound (43.7 mg, 23%) as a pale-yellow solid.

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. additiondiluted with aqueous sodium hydrogen carbonate solution
3. extractionextracted with ethyl acetate
4. washThe organic layer was washed with aqueous sodium hydrogen carbonate solution and saturated brine
5. dry with materialdried over anhydrous magnesium sulfate
6. filtrationfiltrated
7. concentrationThe filtrate was concentrated under reduced pressure
8. customthe residue was purified by silica gel column chromatography (0%→70% ethyl acetate-hexane)