反应详情

4-((4S,5S)-5-(Cyanomethyl)-1-(4-((1-(5-ethoxy-2-fluorophenyl)piperidin-4-yl)oxy)phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl)benzonitrile: To a stirred solution of 4-((4S,5S)-5-(cyanomethyl)-1-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl)benzonitrile (310 mg, 0.970 mmol), 1-(5-ethoxy-2-fluorophenyl)piperidin-4-ol (368 mg, 1.492 mmol) and triphenylphosphine (420 mg, 1.585 mmol) in THF (5.8 mL) at rt was added di-tert-butylazodicarboxylate (375 mg, 1.596 mmol). The resulting solution was stirred at rt for 25 h and then evaporated. The residue was purified by two consecutive chromatographies (SiO2, first 95/5 CHCl3/Ether and then 4/1 to 3/2 Hex/EtOAc) to give the desired product (390 mg, 74.0% yield) as a yellow oil: LC-MS [M+H] 538.

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2. customThe residue was purified by two consecutive chromatographies (SiO2, first 95/5 CHCl3/Ether