反应详情

To a solution of 6-[3-(4-fluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-nicotinic acid (200 mg, 0.58 mmol) in THF (6 mL) was added 1-hydroxybenzotriazole hydrate (90.8 mg, 0.58 mmol), N-ethyldiisopropylamine (254 μL, 1.45 mmol), N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (114 mg, 0.58 mmol) and 2-amino-2-methyl-1-propanol (53.4 mg, 0.58 mmol). The reaction mixture was stirred overnight at room temperature. Chromatography (silica, dichloromethane:methanol=0:100 to 95:5) afforded the title compound (160 mg, 66%) as a colorless oil. MS: m/e=416.2 [M+H]+.