反应详情

To a solution of 6-[3-(4-chloro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-nicotinic acid (224 mg, 0.65 mmol) and 1-methyl-1H-pyrazol-4-ylamine (0.65 mmol) in THF (6 mL) at 0° C. were added 1-hydroxybenzotriazole hydrate (100.8 mg, 0.65 mmol), N-ethyldiisopropylamine (281.7 μl, 1.613 mmol) and N-(3-dimethylaminopropyl)-N′-ethylcarbodiimidazole hydrochloride (126.2 mg, 0.65 mmol). The resulting reaction mixture was stirred overnight at room temperature. Concentration and purification by chromatography (SiO2, heptane:ethyl acetate=3:1 to 1:4) afforded the title compound (201 mg, 73%) which was obtained as a white solid. MS: m/e=424.2 [M+H]+.

1. customThe resulting reaction mixture
2. concentrationConcentration and purification by chromatography (SiO2, heptane:ethyl acetate=3:1 to 1:4)