反应详情

To a solution of 4-(4-bromo-2-fluoro-phenylamino)-6-chloro-pyridazine-3-carboxylic acid tert-butyl ester (300 mg, 0.74 mmol) in DMF (5 ml) under argon at room temperature is added sodium azide (96 mg, 1.48 mmol) with stirring. The reaction mixture is stirred at 50° C. for 6 hours. After cooling to room temperature, the reaction mixture is diluted with ethyl acetate and washed with water, saturated NaHCO3 (20 ml×3) and saturated NaCl (30 ml×3). The organic layer is dried over Na2SO4 and concentrated. The residue is purified by flash column chromatography to provide the desired product.

1. stirringThe reaction mixture is stirred at 50° C. for 6 hours
2. washwashed with water, saturated NaHCO3 (20 ml×3) and saturated NaCl (30 ml×3)
3. dry with materialThe organic layer is dried over Na2SO4
4. concentrationconcentrated
5. customThe residue is purified by flash column chromatography