| 普瑞巴林的合成工艺改进及还原副产物的分离鉴定 |
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| 引用本文： | 陈国华,姚秀梅,柴雨柱,王先登.普瑞巴林的合成工艺改进及还原副产物的分离鉴定[J].中国药物化学杂志,2008,18(6):439-441. |
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| 作者姓名： | 陈国华 姚秀梅 柴雨柱 王先登 |
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| 作者单位： | 1. 中国药科大学,药物化学教研室,江苏,南京,210009
2. 江苏省药物研究所,江苏,南京,210009 |
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| 摘 要： | 目的改进普瑞巴林的合成工艺并分离鉴定还原副产物。方法以亚磷酸三乙酯和氯乙酸乙酯为起始原料,经Arbuzov反应、Wittig-Horner反应、Michael加成、还原、拆分5步反应得到普瑞巴林。结果与结论目标化合物及还原副产物4-异丁基-2-吡咯烷酮经IR1、H-NMR、ESI-MS及元素分析确证,总收率为27.8%,改进后的工艺,反应步骤短,操作安全简便,有利于工业化生产。
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| 关 键 词： | 普瑞巴林 工艺改进 分离鉴定 4-异丁基-2-吡咯烷酮 |
| 收稿时间： | 2008-5-12 |
| 修稿时间： | 2008-9-20 |
Improved synthesis of pregabalin, separation and identification of its by-product |
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| CHEN Guo-hua,YAO Xiu-mei,CHAI Yu-zhu,WANG Xian-deng.Improved synthesis of pregabalin, separation and identification of its by-product[J].Chinese Journal of Medicinal Chemistry,2008,18(6):439-441. |
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| Authors: | CHEN Guo-hua YAO Xiu-mei CHAI Yu-zhu WANG Xian-deng |
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| Institution: | (1.Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China ; 2.Jiangsu Institute of Materia Medica , Nanjing 210009, China ) |
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| Abstract: | Aim To improve the synthetic procedure of pregabalin,separate and identify the by-product.Methods Triethyl phosphite and ethyl chloroacetate were used as starting materials to synthesize pregabalin by Arbuzov reaction,Wittig-Horner reaction,Michael addition,reduction and resolution.Results and conclusion The structures of pregabalin and the by-product 4-isobutylpyrrolidin-2-one were confirmed by IR,1H-NMR,ESI-MS and element analysis.The overall yield is 27.8%.This process has the advantage of less steps and convenient operation,and is suitable for industrial production. |
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| Keywords: | pregabalin process improvement separation and identification 4-isobutylpyrrolidin-2-one |
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