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PROCESS FOR PREPARING 2-PYRROLIDONE DERIVATIVES WITH ONE-SPOT REACTION UNDER MILD REACTION CONDITION

机译:温和反应条件下单点反应制备2-吡咯烷酮衍生物的方法

摘要

PURPOSE: A process for preparing 2-pyrrolidone derivatives is provided, thereby simplifying the process into one-pot reaction, and carrying out the process under mild reaction condition. CONSTITUTION: The process for preparing 2-pyrrolidone derivatives comprises the steps of: reacting 4-amino-3-hydroxybutyric acid or alkyl ester salt thereof with haloacetamide in the presence of organic base in solvent to prepare an intermediate compound; and cyclization of the intermediate compound, wherein R is hydrogen or alkyl; the solvent is selected from dichloromethane, tetrahydrofuran, chloroform, ethylacetate, N,N-dimethylformamide, dimethylsulfoxide and a mixture thereof; the organic base is selected from triethylamine, tributylamine, 1,8-diazabicyclo£5.4.0|undec-7-ene, 1,5-diazabicyclo£4.3.0|non-5-ene and a mixture thereof; and the 2-pyrrolidone derivatives are nootropic agents that enhances reduction of memory, attention or concentration, disorder of language and action, emotional anxiety and enthusiasm deficiency.
机译:目的:提供一种制备2-吡咯烷酮衍生物的方法,从而简化了该方法的一锅法反应,并在温和的反应条件下进行了该方法。组成:2-吡咯烷酮衍生物的制备方法包括以下步骤:在有机碱存在下,使4-氨基-3-羟基丁酸或其烷基酯盐与卤代乙酰胺在溶剂中反应,制得中间体化合物。中间体化合物的环化,其中R是氢或烷基;溶剂选自二氯甲烷,四氢呋喃,氯仿,乙酸乙酯,N,N-二甲基甲酰胺,二甲基亚砜及其混合物;有机碱选自三乙胺,三丁胺,1,8-二氮杂双环£5.4.0 |十一烷基-7-烯,1,5-二氮杂双环£4.3.0 |壬-5-烯及其混合物; 2-吡咯烷酮衍生物是促智药,可增强记忆力,注意力或注意力的集中度,语言和动作障碍,情绪焦虑和热情不足。

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