Sodium Bicarbonate → 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid [(cis)-2-(4-fluoro-phenyl)-cyclopropyl]-amide

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Reaction Steps

cis-2-(4-Fluoro-phenyl)-cyclopropylamine hydrochloride (0.153 g, 0.815 mmol) was dissolved in dichloromethane (4.5 ml) and stirred with NaHCO3 (1 M, 4.5 ml). 3-(difluoromethyl)-1-methyl-1H-pyrazol-4-carbonyl chloride (0.190 g, 0.978 mmol) was added dropwise. After three hours rapid stirring tlc (50% EtOAc/hexane) showed the reaction to be finished. The mixture was separated between dichloromethane and water, washed with NaCl (sat), dried (MgSO4), and evaporated to yield 245 mg of nearly pure product, which was washed with cyclohexane to yield 215 mg (85%) of the product as a white solid m.p. 141-143° C.

Provenance & Evidence