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第 43 卷第 2 期Vol. 43 No. 2
2013 年 4 月Apr 2013

所屬欄目:醫藥及中間體

一鍋法合成2-(3-乙氧基-4-正癸氧基苯胺基)亞甲基丙二酸二乙酯
李志華 (湖南中醫藥高等專(zhuān)科學(xué)校 藥學(xué)系,湖南 株洲 412012)
摘 要:以4-羥基-3-乙氧基苯胺為原料,先與乙氧亞甲叉丙二酸二酯縮合、再與溴癸烷成醚得到2-(3-乙氧基-4-正癸氧基苯胺基)亞甲基丙二酸二乙酯,總收率為89.2%?s合反應在無(wú)溶劑條件下進(jìn)行;癸烷基化反應通過(guò)加水催化,嚴格控制反應體系的含水量在2.0%~5.0%,不僅可以加快反應速率,而且提高了轉化率,避免了催化劑使用,是一條適合生產(chǎn)的新合成工藝路線(xiàn)。
關(guān)鍵詞:2-(3-乙氧基-4-正癸氧基苯胺基)亞甲基丙二酸二乙酯;4-羥基-3-乙氧基苯;合成
中圖分類(lèi)號:S859  文獻標識碼:A  文章編號:1009-9212(2013)02-0055-03
One-pot Synthesis of 3-Ethoxy-4-n-decyloxy-anilionmethylene-malonic Acid Diethyl Ester
LI Zhi-hua (Hunan Traditional Chinese Medical College,Zhuzhou 412012,China)
Abstract:3-Ethoxy-4-n-decyloxy-anilionmethylene-malonic was prepared from 4-hydroxy-5-ethoxyaniline via condensation and etherification in an overall yield of 89.2%. The condensation was conducted in solvent-free solution and the etherification was catalyzed by 2.0%~5.0% of water,which accelerated the reaction speed and increased the conversion. Furthermore,it avoided using the expensive catalyst such as NaI and KI. This novel synthesis route was suitable for large-scale production as it resulted in a simple work-up process and less usage of organic solvent.
Key words:3-Ethoxy-4-n-decyloxy-anilionmethylene-malonic acid diethyl ester;4-Hydroxy-5-ethoxyaniline;Synthesis
作者簡(jiǎn)介:李志華(1981-),女,湖南岳陽(yáng)人,講師,碩士,從事藥物合成以及藥品、食品分析工作。(E-mail:Lzh14084@tom.com)
收稿日期:2013-03-28
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