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注意：请不要用在线翻译，希望能逐句翻译，语法要正确，谢谢！ 【有效期至2008年5月29日】 巴氯芬(Baclofen)，是γ-氨基丁酸的取代衍生物,曾作为肌松药用于临床，近年来又发现了许多新的应用.本实验通过总结以前制备巴氯芬的经验，找出一条新的制备途径。 制备方法：将对氯苯甲醛与丙二酸二乙酯用三乙胺作催化剂缩合生成对氯代苯亚甲基-双-乙酰乙酸乙酯，在氢氧化钠溶液中加热水解得对氯代苯基戊二酸,用乙酐脱水环合生成对氯代苯基戊二酸酐，再用浓氨水胺化生成对氯代苯基戊二酸单酰胺，最后于碱性溶液中滴加次氯酸钠，经Hofmann降解制得巴氯芬。 该合成工艺具有原料易得、反应条件温和、操作简便等优点，从而节省了原料、降低了成本并缩短了反应周期。 [ Last edited by LUOLIYIBIN on 2008-5-28 at 17:22 ] |
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Baclofen (Baclofen), γ-aminobutyric acid is the replacement derivatives, as a muscle relaxant drugs have been used in clinical, in recent years discovered many new applications. This study prepared by summing up past experience baclofen, to find Preparation to a new way. Preparation:-chlorobenzaldehyde and the MDA will Diethyl with triethylamine catalyst for the condensation on the formation of benzene methylene chloride - double - Ethylacetoacetate, sodium hydroxide solution heating hydrolysis The chlorinated phenyl glutaric acid, acetic anhydride dehydration with a generation of chloro phenyl glutaric acid anhydride, and then concentrated on the production of ammonia amine chlorinated phenyl glutaric acid amide, the last in alkaline solution In dropping sodium hypochlorite, as Hofmann degradation system in the baclofen. Synthesis of the raw materials are easily obtained, the mild reaction conditions, easy to operate, and other advantages, saving raw materials and reduce the cost and shorten the reaction cycle. |
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