| 加兰他敏重要中间体溴那维定的合成 |
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| 引用本文： | 杲婷,宋琦,邱银华,张莉莉,史海健.加兰他敏重要中间体溴那维定的合成[J].合成化学,2012,20(2):251-253. |
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| 作者姓名： | 杲婷 宋琦 邱银华 张莉莉 史海健 |
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| 作者单位： | 南京工业大学化学化工学院,江苏南京,210009 |
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| 摘 要： | 以6-溴异香草醛和酪胺为原料,经一锅法进行连续的两步还原胺化制得N-甲基-N-(4-羟基苯乙基)-2-溴-5-羟基-4-甲氧基苯甲胺(4),收率85%。以5%聚乙二醇为相转移催化剂,氯仿为溶剂,铁氰化钾为氧化剂,对4进行氧化偶联,合成了加兰他敏的重要中间体溴那维定,收率39%,其结构经1H NMR,IR和MS确证。
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| 关 键 词： | 加兰他敏 溴那维定 中间体 一锅还原胺化法 氧化偶联 药物合成 |
Synthesis of Important Intermediate Bromonarwedine of Galantamine |
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| GAO Ting
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SONG Qi
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QIU Yin-Hua
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ZHANG Li-Li
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SHI Hai-Jian.Synthesis of Important Intermediate Bromonarwedine of Galantamine[J].Chinese Journal of Synthetic Chemistry,2012,20(2):251-253. |
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| Authors: | GAO Ting SONG Qi QIU Yin-Hua ZHANG Li-Li SHI Hai-Jian |
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| Institution: | (College of Chemical and Chemical Engineering,Nanjing University of Technology,Nanjing 210009,China) |
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| Abstract: | N-methyl-N-(4-hydroxyphenylethyl)-2-bromo-5-hydroxy-4-methoxybenzylamine(4) in 85% yield was prepared by two step sequential reductive amination in "one-pot" method from 6-bromoisovanillin and tyramine.An important intermediate of Galantamine,bromonarwedine(5) in yield of 39%,was synthesized by oxidative coupling reaction of 4 using 5% polyethylene glycol 200 as the phase-transfer catalyst,chloroform as the solvent and potassium ferricyanide as the oxidant. |
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| Keywords: | Galanthamine bromonarwedine intermediate one-pot reductive amination method oxidative coupling drug synthesis |
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