| 吡贝地尔的合成工艺研究 |
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| 引用本文： | 何 湛,徐 静,宋宏锐.吡贝地尔的合成工艺研究[J].中国药物化学杂志,2010,20(4):285-286,297. |
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| 作者姓名： | 何 湛 徐 静 宋宏锐 |
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| 作者单位： | (沈阳药科大学 制药工程学院，辽宁 沈阳 110016) |
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| 摘 要： | 目的 改进吡贝地尔的合成工艺。方法 以邻苯二酚和二氯甲烷为原料经环和反应合成胡椒环，胡椒环与多聚甲醛经Blanc氯甲基化反应合成重要中间体胡椒基氯(3)；以哌嗪和二氯嘧啶为原料经氮烷基化反应合成重要中间体1-(2-嘧啶基)哌嗪(4)；(3)和(4)经氮烷基化反应得到目标化合物。结果与讨论 目标化合物的结构经1H-NMR、GC-MS谱确证，总收率为44.2%，改进后的工艺操作简便，成本低廉，有利于工业化生产。
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| 关 键 词： | 吡贝地尔 多巴胺能激动剂 帕金森病 工艺改进 |
| 收稿时间： | 2010-1-14 |
| 修稿时间： | 2010-5-20 |
Improved synthesis of piribedil |
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| HE Zhan,XU Jing,SONG Hongrui.Improved synthesis of piribedil[J].Chinese Journal of Medicinal Chemistry,2010,20(4):285-286,297. |
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| Authors: | HE Zhan XU Jing SONG Hongrui |
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| Institution: | (School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China) |
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| Abstract: | Aim To improve the procedure of piribedil.Methods The intermediate piperonyl chloride（3） was obtained through cyclization and Blanc reaction by using o-dihydroxybenzene and dichloromethane as starting material.Another intermediate 1-（2-pyrimidyl）piperazine（4） was obtained through N-alkylation by using 2-chloropyrimidine and piperazine as starting material.After N-alkylation between intermediates（3） and（4）,piribedil could be obtained.Results and conclusion The structure of piribedil was confirmed by 1H-NMR,GC-MS.The overall yield is 44.2%.The improved process has the advantage of low cost and it is also suitable for industrial production. |
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| Keywords: | piribedil dopaminergic agonist Parkinson′s disease process improvement |
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