2-(4-哌啶基)乙醇的合成工艺的研究

Research on Synthesis of 2-(piperidin-4-yl)Ethanol

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-（Piperidin-4-yl） ethanol is a very important intermediate of pipothiazine which is the representative drug of anti-psychotic disorders. In this paper, 1-benzylpiperidin-4-one was condensed by Wittig reagent, and then reduced by LiAlH4 and Ni to give the final target compounds. Effects of different reducing agent proportion, reaction temperature on the yield of the LiAlH4 reduction process were studied as well as effects of Ni proportion, reaction press and reaction temperature on the yield of Ni reduction process. Under optimized conditions, the total yield could reach up to 55.7%, the reaction condition was mild, and the post processing was easily. At last, the structure of target compound was confirmed by means of ESI-MS and ^1HNMR.