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2-(4-哌啶基)乙醇是治疗精神分裂药物哌泊噻嗪的一个关键中间体。本文以苄基哌啶酮为起始原料,经Wittig反应,四氢铝锂低温还原、兰尼镍还原脱苄基反应得到目标化合物。并考察了四氢铝锂还原反应还原剂的用量、反应温度,兰尼镍还原反应还原剂的用量、反应压强、反应温度对反应收率的影响。优化后3步反应总收率可达55.7%,且反应条件温和,后处理简便,产品经ESI-MS和1HNMR确证结构。
2- (4-piperidinyl) ethanol is a key intermediate for the treatment of the pipazothiazine, a schizophrenic drug. In this paper, benzylpiperidone as the starting material, Wittig reaction, lithium aluminum hydride reduction, Lan Ni nickel reduction debenzylation reaction of the target compound. The effects of the amount of reductant, the reaction temperature, the amount of reductant, the pressure of reaction and the reaction temperature on the yield of lithium aluminum hydride reduction reaction were investigated. After the optimization, the total yield of the three-step reaction reached 55.7%. The reaction conditions were mild and the post-treatment was simple. The structure of the product was confirmed by ESI-MS and 1HNMR.