Water → 1-(Methylsulfonyl)-1H-pyrazol-4-amine

Participants

Reaction Steps

To a solution of 4-nitro-1H-pyrazole (250 mg, 2.2 mmol) in DCM (5 mL) were added triethylamine (0.46 mL, 1.5 eq) and methanesulfonyl chloride (0.20 mL, 1.2 eq). After stirring for 1 h at rt, water was added and the aqueous phase extracted with DCM. The combined organic phases were dried over sodium sulfate and concentrated in vacuo. The residue was dissolved in 5 mL methanol and palladium on carbon added under an inert atmosphere. The reaction mixture was stirred overnight at rt under an hydrogen atmosphere. The resulting mixture was filtered through Celite and the filtrate concentrated in vacuo to give 1-(methylsulfonyl)-1H-pyrazol-4-amine as a brown oil (0.34 g, 2.1 mmol, 96%).

Provenance & Evidence