反应详情

3-[(Piperidin-4-yl)carbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (100 mg) obtained in Example 228 is dissolved in N,N-dimethylformamide (3 ml), and thereto are added successively nicotinic acid (34 mg), 1-hydroxybenzotriazole (37 mg) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (53 mg), and the mixture is stirred at room temperature for 4 hours. To the reaction solution are poured a saturated aqueous sodium hydrogen carbonate solution and water, and the precipitates are collected by filtration, washed with chloroform, and dried to give 3-[1-((pyridin-3-yl)carbonyl)piperidin-4-ylcarbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (103 mg). This product is treated with hydrogen chloride in dioxane to give the title compound (115 mg).

1. filtrationthe precipitates are collected by filtration
2. washwashed with chloroform
3. customdried