Potassium Hydroxide → HCID 123151441, compound

Participants

Reaction Steps

A mixture of 4-(2-methoxyvinyl)-1-methyl-1H-pyrazol-3-amine a17-1 (500 mg, 3.27 mmol, 1 eq), 5-bromovaleryl chloride (651.9 mg, 3.27 mmol, 1 eq), potassium hydroxide (550.1 mg, 9.80 mmol, 3 eq), 4-dimethymaminopyridine (39.9 mg, 0.33 mmole, 0.1 eq) and N,N,N-tributylbutan-1-aminium bromide (105.3 mg, 0.33 mmole, 0.1 eq) in toluene (15 ml) is heated to reflux overnight. After filtration and evaporation the residue is purified by reverse phase chromatography (basic mode, gradient: H2O/acetonitrile/NH4OH from 80/20/0.1 to 50/50/0.1 in 10 minutes) to afford 1-[4-(2-methoxyvinyl)-1-methyl-1H-pyrazol-3-yl]piperidin-2-one a17-2.

Provenance & Evidence