| 地诺孕素的合成 |
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| 引用本文： | 梁勇,陈博,王绍杰.地诺孕素的合成[J].沈阳药科大学学报,2011,28(10):788-790. |
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| 作者姓名： | 梁勇 陈博 王绍杰 |
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| 作者单位： | 辽宁海思科制药有限公司;沈阳药科大学制药工程学院; |
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| 摘 要： | 目的研究地诺孕素的合成方法。方法以雌甾-4,9-二烯-3,17-二酮(1)为原料,首先用2,2-二甲基-13,-丙二醇对3位羰基进行保护,再经过环氧化、氰化开环、脱保护制得17α-氰甲基-17β-羟基-13β-甲基甾烷-4,9-二烯-3-酮,即地诺孕素(5)。结果目标化合物结构经1H-NMR1、3C-NMR、MS和IR确证结构,总收率45.5%。结论新工艺原料易得、操作简便、反应条件温和,有一定的工业生产应用价值。
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| 关 键 词： | 地诺孕素 22 -二甲基-1 3-丙二醇 合成 |
| 收稿时间： | 2011-4-28 |
| 修稿时间： | 2011-7-8 |
Synthesis of dienogest |
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| LIANG Yong,CHEN Bo,WANG Shao-jie.Synthesis of dienogest[J].Journal of Shenyang Pharmaceutical University,2011,28(10):788-790. |
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| Authors: | LIANG Yong CHEN Bo WANG Shao-jie |
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| Institution: | LIANG Yong1,CHEN Bo2,WANG Shao-jie2(1.Liaoning Haisco Pharmaceutical Co.,LTD.,Xingcheng 125107,China,2.School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China) |
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| Abstract: | Objective To research the synthetic procedure of dienogest. Methods Dienogest was prepared from estra-4,9-diene-3,17-dione,2,2-dimethylpropane-1,3-diol via 3-position ketalation,17-epoxidation,ring cleavage and 3-position hydrolysis reactions. Results The structure of target compound was confirmed by 1H-NMR,13C-NMR,MS and IR.The overall yield was 45.5%. Conclusions The process should have certain value for industrial application considering its availability of the raw materials,simple operation and mild rea... |
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| Keywords: | dienogest 2 2-dimethylpropane-1 3-diol synthesis |
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