反应详情

温度

80 °C

3-(2-Methylcyclopropyl)-3-oxopropanenitrile (0.240 g, 1.95 mmol) was dissolved in dry ethanol (3 mL). Hydrazine monohydrate (0.728 mL, 9.75 mmol) was added, and the reaction mixture was heated to 80° C. for 20 minutes. The reaction mixture was then cooled to room temperature and concentrated. Silica gel chromatography (5% MeOH/DCM) provided a mixture of cis and trans isomers which were separated by chiral HPLC providing 3-(cis-2-methylcyclopropyl)-1H-pyrazol-5-amine (74 mg, 28% for two steps) as an oil.

1. temperatureThe reaction mixture was then cooled to room temperature
2. concentrationconcentrated
3. customSilica gel chromatography (5% MeOH/DCM) provided
4. additiona mixture of cis and trans isomers which
5. customwere separated by chiral HPLC