反应详情

To a solution of N-[6-(4-amino-2-fluorophenoxy)imidazo[1,2-a]pyridin-2-yl]cyclopropanecarboxamide (150 mg, 0.460 mmol) in N,N-dimethylacetamide (3.0 mL) were added 1-[(4-fluorophenyl)carbamoyl]cyclopropanecarboxylic acid (154 mg, 0.689 mmol), HATU (262 mg, 0.689 mmol) and N,N-diisopropylethylamine (120 μL, 0.689 mmol), and the mixture was stirred at room temperature for 4 hr. Saturated aqueous sodium hydrogen carbonate was added to the reaction mixture, and the mixture was extracted with ethyl acetate/tetrahydrofuran. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate and filtered. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane/ethyl acetate=40/60→0/100), washed with hexane/ethyl acetate and collected by filtration to give the title compound (99 mg, 41%) as a white solid.

1. extractionthe mixture was extracted with ethyl acetate/tetrahydrofuran
2. washThe organic layer was washed with saturated brine
3. dry with materialdried over anhydrous magnesium sulfate
4. filtrationfiltered
5. customThe solvent was evaporated under reduced pressure
6. customthe residue was purified by silica gel column chromatography (hexane/ethyl acetate=40/60→0/100)
7. washwashed with hexane/ethyl acetate
8. filtrationcollected by filtration