反应详情

In a 25 mL flask was added 455 mg of 4-(4-chloro-phenyl)-piperidine-4-carbonitrile (2.06 mmol, 1.0 equiv), 500 mg of (4-chloro-5-methyl-3-trifluoromethyl-pyrazol-1-yl)-acetic acid (2.06 mmol, 1.00 equiv), 1.10 g of BOP (2.47 mmol, 1.2 equiv), 1.15 mL TEA (8.24 mmol, 4.00 equiv) and 6 mL NMP. A stir bar was placed in the flask and the reaction solution was stirred overnight at room temperature under N2 atmosphere. The crude product was purified by normal phase HPLC (EtOAc-hexane as the eluent) to yield 1-[2-(4-chloro-5-methyl-3-trifluoromethyl-pyrazol-1-yl)-acetyl]-4-(4-chloro-phenyl)-piperidine-4-carbonitrile: MS (ES) M+H expected=445.3, found=445.1.

1. customA stir bar was placed in the flask
2. customThe crude product was purified by normal phase HPLC (EtOAc-hexane as the eluent)