| 依帕司他的合成工艺研究 |
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| 引用本文： | 李月珍,赖宜生,梁臣艳. 依帕司他的合成工艺研究[J]. 中国药物化学杂志, 2001, 11(3): 165-167 |
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| 作者姓名： | 李月珍 赖宜生 梁臣艳 |
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| 作者单位： | 1. 广西南宁地区教育学院化学系,
2. 广西中医学院药物化学教研室, |
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| 摘 要： | 以甘氨酸和二硫化碳为起始原料，经加成、取代、环合、缩合四步反应合成了依帕司他。在加成反应中采用相转移催化法，使3－羟甲基绕丹宁收率提高到85．3％，合成总收率达到55．8％。该合成工艺操作简便，收率较高，在加成反应中避免使用有机溶剂。
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| 关 键 词： | 依帕司他 醛糖还原酶抑制剂 3－羟甲基绕丹宁 相转移催化剂 合成 |
| 文章编号： | 1005-0108(2001)03-0165-03 |
A Study on the SyntheticTechnology of Epalrestat |
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| LI Yue-zhen,LAI Yi-sheng,LIANG Chen-yan. A Study on the SyntheticTechnology of Epalrestat[J]. Chinese Journal of Medicinal Chemistry, 2001, 11(3): 165-167 |
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| Authors: | LI Yue-zhen LAI Yi-sheng LIANG Chen-yan |
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| Affiliation: | LI Yue-zhen 1,LAI Yi-sheng 2,LIANG Chen-yan 2 |
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| Abstract: | Epalrestat was synthesized through addition,substitution,cylization and condensation from the starting material glycine and carbon disulfide.In the addition procedure,a phase transfer catalyst was used,the yield of the intermediate 3-carboxymethyl rhodanine was raised to 85 3% and the overall yield was 55 8%.This synthesis had the advantages of easier operation,higher yield,and avoided using organic solvents in the addition procedure. |
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| Keywords: | epalrestat aldose reductase inhibitor 3-carboxymethyl rhodanine phase transfer catalyst synthesis |
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