3-Cyanobenzoic acid → Tert-butyl 4-(3-cyanobenzoyl)piperazine-1-carboxylate

Participants

Reaction Steps

DIEA (527 mg, 4.07 mmol), HOBt (322 mg, 2.45 mmol), EDCI.HCl (302 m, 1.5 mmol) and piperazine-1-carboxylic acid tert-butyl ester (456 mg, 2.45 mmol) were added to a stirred solution of 3-cyano-benzoicacid (300 mg, 2.03 mmol) in DMF (3 mL) and the resulting mixture was stirred at ambient temperature overnight. The reaction mixture was then diluted with water and the product was extracted with ethyl acetate. The ethyl acetate layer was washed with brine solution, dried over Na2SO4, and concentrated under reduced pressure to afford 590 mg (92%) of 4-(3-cyano-benzoyl)-piperazine-1-carboxylic acid tert-butyl ester.

Provenance & Evidence