反应详情

(E)-2-[2-(1H-indazol-3-yl)vinyl]phenylamine (60 mg, 0.26 mmol) was dissolved in THF (5 mL) and the solution was added with 2-pyrazinecarboxylic acid (38 mg, 0.31 mmol), 1-hydroxybenzotriazole monohydrate (51 mg, 0.33 mmol), 4-methylmorpholine (47 μL, 0.51 mmol) and EDC (68 mg, 0.36 mmol), followed by stirring at room temperature for 3 hours. The reaction mixture was added with saturated aqueous sodium hydrogencarbonate solution and extracted with ethyl acetate. The organic layer was sequentially washed with water and saturated brine, dried over anhydrous magnesium sulfate and the solvent was evaporated under reduced pressure. The residue was triturated in ethanol to obtain Compound 28 (25 mg, 30%).

1. extractionextracted with ethyl acetate
2. washThe organic layer was sequentially washed with water and saturated brine
3. dry with materialdried over anhydrous magnesium sulfate
4. customthe solvent was evaporated under reduced pressure
5. customThe residue was triturated in ethanol