1H-Pyrazol-3-amine, 5-(1-methylcyclopropyl)- synthesis

Yield:503568-73-8 28%

Reaction Conditions:

with hydrazine hydrate in ethanol at 80; for 0.5 h;

Steps:

20.A

3-(l-Methyl-cyclopropyl)-3-oxo-propionitrile (1.0 g, 8.12 mmol) was dissolved in EtOH (10 niL). Hydrazine monohydrate (3.03 mL, 40.6 mmol) was added, and the reaction mixture was heated to 80°C for 30 minutes and then cooled to room temperature. The reaction was concentrated and purified by column chromatography eluting with EtOAc to give 3-(l-methylcyclopropyl)-lH-pyrazol-5-amine as an oil (311 mg, 28% yield).

References:

WO2011/25968,2011,A1 Location in patent:Page/Page column 61