反应详情

To a stirred solution of 4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxylic acid, 8-b, (200 mg, 0.97 mmol) and DIEA (380 mg, 2.91 mmol) in DMF (3 ml) was added HATU (370 mg, 0.97 mmol). The mixture was stirred for 5 min at room temperature and then compound 20-e (351 mg, 0.97 mmol) was added. The resulting mixture was stirred at 60° C. for 3 hour. The mixture was then diluted with water and extracted with ethyl acetate. The organic layer was washed with brine, dried over sodium sulfate and concentrated under vacuum. The residue was purified on silica gel chromatography (dichloromethane:methanol=20/1) to provide the product, 20-f, (400 mg, 80%).

1. stirringThe resulting mixture was stirred at 60° C. for 3 hour
2. extractionextracted with ethyl acetate
3. washThe organic layer was washed with brine
4. dry with materialdried over sodium sulfate
5. concentrationconcentrated under vacuum
6. customThe residue was purified on silica gel chromatography (dichloromethane:methanol=20/1)