反应详情

A mixture of N-(1-cyano-piperidin-4-yl)-N-cyclopropyl-4-oxazol-5-yl-benzamide (200 mg), hydroxylamine hydrochloride (70 mg), and potassium carbonate (82 mg) in ethanol (0.70 mL) and water (1.00 mL) is heated under reflux for 5 h. The reaction mixture is cooled to room temperature, stirred at this temperature for two days and concentrated in vacuo. The residue is mixed with water and ethyl acetate and the organic phase is separated, dried and concentrated in vacuo. The crude product is purified by HPLC (MeOH/H2O/TFA). LC (method 3): tR=1.35 min; Mass spectrum (ESI+): m/z=370 [M+H]+.

1. temperatureis heated
2. temperatureunder reflux for 5 h
3. concentrationconcentrated in vacuo
4. additionThe residue is mixed with water and ethyl acetate
5. customthe organic phase is separated
6. customdried
7. concentrationconcentrated in vacuo
8. customThe crude product is purified by HPLC (MeOH/H2O/TFA)