反应详情

To a solution of 6-[3-(4-fluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-nicotinic acid (100 mg, 0.29 mmol) in THF (3 mL) were added 1-hydroxybenzotriazole hydrate (45.3 mg, 0.29 mmol), N-ethyldiisopropylamine (127 μL, 0.73 mmol), N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (56.7 mg, 0.29 mmol) and 1-methyl-1H-pyrazol-4-ylamine (28.2 mg, 0.29 mmol). The reaction mixture was stirred overnight at room temperature. Chromatography (silica, ethyl acetate:heptane=2:1 to 9:1) afforded the title compound (70 mg, 57%) as a white solid. MS: m/e=424.2 [M+H]+.