| 新型镇静催眠药茚地普隆的合成 |
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| 引用本文： | 樊士勇,米春来,何新华,李松,郑志兵.新型镇静催眠药茚地普隆的合成[J].中国药物化学杂志,2006,16(6):363-365. |
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| 作者姓名： | 樊士勇 米春来 何新华 李松 郑志兵 |
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| 作者单位： | 军事医学科学院,毒物药物研究所,北京,100850 |
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| 摘 要： | 目的 改进茚地普隆的合成工艺.方法 以3-氨基苯乙酮为起始原料,经3步反应制得N-3-(3-二甲基胺)-1-氧-2-丙烯基]-苯基-N-甲基]-乙酰胺(4);以2-乙酰噻吩为起始原料,经4步反应制得(3-氨基-1H-吡唑-4-基)-2-噻吩基甲酮(8),4和8在冰醋酸介质中加热关环得到茚地普隆.结果与结论 改进了茚地普隆的合成工艺,产物结构经MS、1H-NMR以及元素分析确证,总收率为36.0%.
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| 关 键 词： | 药物化学 药物制备 工艺改进 茚地普隆 镇静催眠药 |
| 文章编号： | 1005-0108（2006）06-0363-03 |
| 收稿时间： | 2006-05-29 |
| 修稿时间： | 2006年5月29日 |
Synthesis of a novel sedative-hypnotic indiplon |
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| FAN Shi-yong,MI Chun-lai,HE Xin-hua,LI Song,ZHENG Zhi-bing.Synthesis of a novel sedative-hypnotic indiplon[J].Chinese Journal of Medicinal Chemistry,2006,16(6):363-365. |
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| Authors: | FAN Shi-yong MI Chun-lai HE Xin-hua LI Song ZHENG Zhi-bing |
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| Institution: | Institute of Pharmacology and Toxicology, Academy of Military Medical Science, Beijing 100850, China |
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| Abstract: | Aim To improve the synthetic procedure of indiplon.Methods N-3-3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-N-methylacetamide(4) was synthesized from 3-aminoacetophenone via three steps.(3-Amino-1H-pyrazol-4-yl)-2-thienyl-methanone(8) was synthesized from 2-acetylthiophene via four steps.Indiplon(1) was obtained by the reaction between 4 and 8 in the presence of glacial acetic acid.(Results and conclusion) The structure of target compound was confirmed by MS,()~1H-NMR and element analysis.The total yield was 36.0%.The easily available and cheap starting material was used to synthesize indipolon.The purification method of the target compound was improved. |
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| Keywords: | medicinal chemistry drug preparation chemical synthesis indiplon sedative-hypnotic drug |
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