Potassium Phosphate, Tribasic → 4-(5-Cyclopropylpyridin-2-yl)piperazine-1-carboxylic acid tert-butyl ester

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Reaction Steps

To a mixture of 4-(5-bromopyridin-2-yl)piperazine-1-carboxylic acid tert-butyl ester (5.37 g), bis(tricyclohexylphosphine)palladium (II) dichloride (347 mg), tripotassium phosphate (9.99 g) and cyclopropylboronic acid (2.02 g) were added toluene (49 mL) and water (2.5 mL), and the mixture was refluxed. After cooling, ethyl acetate and saturated aqueous sodium hydrogen carbonate solution were added, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over sodium sulfate, and the solvent was evaporated. The residue was purified by column chromatography (hexane:ethyl acetate) to give the title compound (3.41 g).

Provenance & Evidence