反应详情

To a stirred solution of 4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxylic acid, 8-b, (7.9 g, 25.7 mmol) and Et3N (7.09 g, 70.2 mmol) in MeCN (50 ml) was added HATU (10.7 g, 28.2 mmol). The mixture was stirred for 10 min at room temperature and then ethyl 3-((R)-amino(phenyl)methyl)phenyl(methyl)phosphinate, 24-e, (6.79 g, 23.4 mmol) was added. The resulting mixture was stirred at room temperature for 1 hour. The mixture was then concentrated under vacuum and the residue was taken into ethyl acetate followed by washing with saturated NH4Cl. The organic layer was dried over sodium sulfate and concentrated under vacuum to provide the crude product, 24-f, (18.8 g) as red oil. The crude product was used for the next step directly.

1. stirringThe resulting mixture was stirred at room temperature for 1 hour
2. concentrationThe mixture was then concentrated under vacuum
3. washby washing with saturated NH4Cl
4. dry with materialThe organic layer was dried over sodium sulfate
5. concentrationconcentrated under vacuum