4-(Bromomethyl)benzonitrile → 1-[2-(4-Cyanobenzyloxy)ethyl]-3-[2-(2,2,2-trifluoroethyl)guanidino]pyrazole

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Reaction Steps

A mixture of 1-(2-hydroxyethyl)-3-[2-(2,2,2-trifluoroethyl)guanidino]pyrazole (2.51 g.) and p-cyanobenzyl bromide (1.96 g.) was heated at 140° for 10 minutes. The melt, on cooling, was dissolved in MeOH (5 ml.) and purified by chromatography on silica gel using EtOAc/EtOH/triethylamine 9:1:1 v/v/v as eluant to give 4-(2-[3-(2-[2,2,2-trifluoroethyl]guanidino)pyrazol-1-yl]ethoxymethyl)benzonitrile (700 mg.; 19%).

Provenance & Evidence