反应详情

To a solution of 5-methyl-1-phenyl-1H-pyrazole-3-carboxylic acid (197 mg, 973 μmol) in tetrahydrofuran (2 mL) were added oxalyl chloride (80 μL, 973 μmol) and N,N-dimethylformamide (2 drops) under ice-cooling, and the mixture was stirred at room temperature for 1 hr. A solution of N-[6-(4-aminophenoxy)imidazo[1,2-a]pyridin-2-yl]cyclopropanecarboxamide (200 mg, 649 μmol) in N,N-dimethylacetamide (2 mL) was added to the reaction solution, and the mixture was stirred at room temperature for 2 hr. Saturated aqueous sodium hydrogen carbonate was added to the reaction solution, and the mixture was extracted with ethyl acetate. The organic layer was washed with 1N aqueous sodium hydroxide solution, water and saturated brine, dried over anhydrous magnesium sulfate and concentrated. The obtained residue was recrystallized from ethanol/water to give the title compound (187 mg, 39%) as a white powder.

1. temperaturecooling
2. stirringthe mixture was stirred at room temperature for 2 hr
3. extractionthe mixture was extracted with ethyl acetate
4. washThe organic layer was washed with 1N aqueous sodium hydroxide solution, water and saturated brine
5. dry with materialdried over anhydrous magnesium sulfate
6. concentrationconcentrated
7. customThe obtained residue was recrystallized from ethanol/water