| 米格列奈中间体顺式全氢异吲哚的合成工艺改进 |
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| 引用本文： | 虞春晓,朱雄,王尔华,汪会海. 米格列奈中间体顺式全氢异吲哚的合成工艺改进[J]. 药学进展, 2006, 30(4): 179-181 |
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| 作者姓名： | 虞春晓 朱雄 王尔华 汪会海 |
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| 作者单位： | 中国药科大学医药化工研究所,江苏,南京,210009 |
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| 摘 要： | 目的：改进米格列奈的重要中间体顺式全氢异吲哚的合成工艺。方法：将顺式六氢邻苯二甲酸酐和尿素反应，得顺式六氢邻苯二甲酰亚胺，再经氢化铝锂还原两个羰基，合成顺式全氢异吲哚。结果：合成得到目标产物，纯度大于98％，两步反应的总收率达56．3％，其结构经^1HNMR和ESI-MS确证。结论：该合成工艺所用原料易得，反应条件温和，产物纯度和收率高，适合于工业化生产。
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| 关 键 词： | 米格列奈 顺式全氢异吲哚 中间体 合成 |
| 文章编号： | 1001-5094（2005）04-0179-03 |
| 收稿时间： | 2005-12-29 |
| 修稿时间： | 2005-12-29 |
An Improved Synthesis Method of Cis-hexahydroisoindoline,the Intermediate of Mitiglinide |
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| YU Chun-xiao,ZHU Xiong,WANG Er-hua,WANG Hui-hai. An Improved Synthesis Method of Cis-hexahydroisoindoline,the Intermediate of Mitiglinide[J]. Progress in Pharmaceutical Sciences, 2006, 30(4): 179-181 |
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| Authors: | YU Chun-xiao ZHU Xiong WANG Er-hua WANG Hui-hai |
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| Affiliation: | Medicinal and Chemical Institute, China Pharmaceutical University, Nanjing 210009, China |
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| Abstract: | Objective:To improve the synthesis method of cis-hexahydroisoindoline,an important intermediate of mitiglinide.Methods:Cis-hexahydrophthalic anhydride reacted with urea to obtain cis-hexahydrophthalimide,followed by reduction reaction with lithium-aluminum hydride to remove the two carbonyls,to obtain target compound.Results:The target compound was synthesized,its purity was more than 98% and the total yield was 56.3%.Its structure was confirmed by(()~(1)HNMR) and ESI-MS.Conclusion:The materials used for the improved synthesis are easily obtained,the reaction conditions are very moderate,and the product purity and yield are increased in improved synthesis.This synthesis method is suitable for industry. |
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| Keywords: | Mitiglinide Cis-hexahydroisoindoline Intermediate Synthesis |
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