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To a vial containing the 2-piperazin-l-yl-benzoic acid methyl ester (0.667 g, 3.03 mmol) is added a pre-mixed solution containing (3,5-dimethyl-pyrazol-l-yl)-acetic acid (0.428 g, 2.78 mmol) and carbonyl dimidazole (0.567 g, 3.50 mmol). The mixture is stirred overnight and then diluted with 200 mL of EtOAc followed by 200 mL of saturated NH4Cl. The organic phase is washed with 2x200 mL of H2O and 1x200 mL of brine, dried (MgSO4), filtered and concentrated to give 0.849 g of 2-{4-[2-(3,5-dimethyl- pyrazol-l-yl)-acetyl]-piperazin-l-yl} -benzoic acid methyl ester in 86% yield.
With N-ethyl-N,N-diisopropylamine; 1,1'-carbonyldiimidazole; In N,N-dimethyl-formamide; at 20℃;
To a vial containing the 2-piperazin-l-yl-benzoic acid methyl ester (0.667 g, 3.03 mmol) is added a pre-mixed solution containing (3,5-dimethyl-pyrazol-l-yl)-acetic acid (0.428 g, 2.78 mmol) and carbonyl diimidazole (0.567 g, 3.50 mmol). The mixture is stirred overnight and then diluted with 200 mL of EtOAc followed by 200 mL of sat. NH4Cl. The organic phase is washed with 2 x 200 mL of H2O and 1 x 200 mL of brine. The organic phase is dried with MgSO4, filtered and concentrated to give 0.849 g of 2-{4-[2- (3,5-dimethyl-pyrazol-l-yl)-acetyl]-piperazin-l-yl} -benzoic acid methyl ester.
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