1-Hydroxybenzotriazole → (4-Bromo-2,6-difluorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

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Reaction Steps

4-Bromo-2,6-difluorobenzoic acid (2.875 g) and 1-(3,5-dimethylpyridin-2-yl)piperazine (2.32 g) described in Preparation Example 47 and 1-hydroxybenzotriazole 1hydrate (1.64 g) were dissolve in N,N-dimethylformamide (50 mL), 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride (2.32 g) was added, and the mixture was stirred at room temperature overnight. To the reaction mixture was added saturated brine, and the mixture was extracted with ethyl acetate. The organic layer was washed with water and saturated brine, and the solvent was evaporated. The residue was purified by column chromatography (chloroform:methanol) to give the title compound (4.33 g).

Provenance & Evidence