反应详情

A solution of (E)-2-[2-(1H-indazol-3-yl)vinyl]benzoic acid (30 mg, 0.11 mmol) obtained in Step 1 of Example 47 in THF (0.50 mL) was sequentially added with 4-methylmorpholine (25 μL, 0.23 mmol), 3-amino-1,2,4-triazole (14 mg, 0.17 mmol), EDC (31 mg, 0.16 mmol) and 1-hydroxybenzotriazole monohydrate (20 mg, 0.15 mmol) followed by stirring at room temperature for 2.0 hours. The reaction mixture was added organic layer and aqueous layer and the organic layer was with water and ethyl acetate to separate the mixture into concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform/methanol=100/0 to 90/10) to obtain Compound 139 (17 mg, 45%).

1. additionThe reaction mixture was added organic layer and aqueous layer
2. customto separate the mixture
3. concentrationinto concentrated under reduced pressure
4. customThe residue was purified by silica gel column chromatography (chloroform/methanol=100/0 to 90/10)