反应详情

3-[(Piperidin-4-yl)carbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (140 mg) obtained in Example 228 is suspended in dichloromethane (10 ml), and thereto are added acetyl chloride (30 μl) and triethylamine (74 μl) under ice-cooling, and the mixture is stirred at room temperature for 6 hours. The reaction solution is diluted with chloroform, washed successively with water, 5% aqueous citric acid solution, a saturated aqueous sodium hydrogen carbonate solution and a saturated brine, and dried over sodium sulfate. The solvent is evaporated under reduced pressure, and the resulting residue is dissolved in ethyl acetate, and treated with activated carbon. The resulting residue is recrystallized from ethyl acetate to give the title compound (38 mg).

1. temperaturecooling
2. washwashed successively with water, 5% aqueous citric acid solution
3. dry with materiala saturated aqueous sodium hydrogen carbonate solution and a saturated brine, and dried over sodium sulfate
4. customThe solvent is evaporated under reduced pressure
5. dissolutionthe resulting residue is dissolved in ethyl acetate
6. additiontreated with activated carbon
7. customThe resulting residue is recrystallized from ethyl acetate