反应详情

To a stirred suspension of (S)-4-(5-(4-(4-fluorophenyl)-2-oxooxazolidin-3-yl)pyrazolo[1,5-a]pyrimidin-3-yl)benzohydrazide (0.062 g, 0.14 mmol) in 2:1 THF-DMF (1.5 mL) was added triethylamine (0.026 mL, 0.19 mmol), followed by ethyl acetimidate hydrochloride (0.021 g, 0.17 mmol) at 0° C. The mixture was allowed to warm up to ambient temperature and stirring continued at 60° C. for 5 hours. The mixture was poured into water, neutralized with 1N HCl, extracted with EtOAc, dried (phase separator silicone treated filter paper) and concentrated to give (S)-4-(5-(4-(4-fluorophenyl)-2-oxooxazolidin-3-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-N′-(1-iminoethyl)benzohydrazide (0.049 g, 72% yield) as a yellow oil.

1. extractionextracted with EtOAc
2. customdried
3. addition(phase separator silicone treated filter paper)
4. concentrationconcentrated