N-叔队搿与氧羰基哌嗪制备工艺研究.doc

中银3 -哌啶酮 中科院NO.98977 - 36 - 7 复合标识的H - N0191 -叔- 2 -氨甲基哌啶 中科院NO.370069 - 31 - 1 复合标识的H - N010CAS NO.1 -叔丁氧哌啶- 2 -羧酸阿哲... 中科院NO.98303 - 20 – 91 -叔丁氧哌啶- 3 -羧基阿哲... 中科院NO.84358 - 12 – 3叔丁氧哌啶- 4 -羧酸阿哲... 中科院NO.84358 - 13 – 4哌啶N-叔丁氧羰基哌嗪制备工艺研究摘要 摘 要 本文介绍了 N-叔丁氧羰基哌嗪，它是属于哌嗪类单取代化合物。此类药物 与传统有机药物相比较具有高效的药理活性。在有机合成中，作为活泼的医药中 间体，可进一步合成许多类型的有机化合物。具有很强的研究意义。 N-叔丁氧羰基哌嗪合成是由哌嗪出发，与冰醋酸发生成盐反应，无水乙醇作 为溶剂，再加入二碳酸二叔丁酯通过酰化反应得到 N-叔丁氧羰基哌嗪粗品。在 反应过程中需要严格控制 pH 值和温度，以此来减少副产物的生成。后处理中， 以乙酸乙酯为萃取剂，除去未反应的原料与其他杂质。最后得到合格的 N-叔丁 氧羰基哌嗪产品。 经实验过程分析， 实验数据验证。 得出 N-叔丁氧羰基哌嗪的一些物化性质， 可以看出此工艺具有一定的可行性，产品质量稳定，优于其它工艺路线。有着广 阔的市场效益和经济利润。 关键词： 关键词：N-叔丁氧羰基哌嗪； 哌嗪； 二碳酸二叔丁酯； 医药中间体； I 摘要 Abstract This article describes the N-tert-butoxycarbonyl piperazine, it belongs to a single substituted piperazine compounds. These drugs compared with traditional organic drugs with high pharmacological activity. In organic synthesis, as the active pharmaceutical intermediates, further synthesis of many types of organic compounds. Research has a strong meaning. N-tert-butoxycarbonyl piperazine piperazine synthesized by starting with the acetic acid salt reaction occurs, anhydrous ethanol as solvent, then add the second di-tert-butyl carbonate obtained by acylation of N-tert-butoxycarbonyl piperazine crude. In the reaction process, the need for strict control of pH value and temperature, in order to reduce the by-product formation. After treatment with ethyl acetate as extracting agent to remove unreacted raw materials, isomers and by-products and other impurities. Finally, access to qualified N-Boc piperazine-based products. The experimental process analysis, experimental data. Obtained N-tert-butoxycarbonyl piperazine some of the physical and chemical properties, can be seen that this process is feasible, stable product quality, better than the other process routes. Has a broad market efficiency and economic profit. Key words: N-tert-butoxycarbonyl piperazine; piperazine; two-di-tert butyl carbonate; pharmaceutical intermediates; II 目录 目