《中枢兴奋药茴拉西坦的合成研究》》-毕业论文.docVIP

济南大学毕业设计 2 - 精品 精品 毕业论文 题 目 中枢兴奋药茴拉西坦的合成研究 学 院 医学与生命科学学院 专 业 制药工程 班 级 0801班 学 生 学 号 20080209050 指导教师 二〇一 二 年 五 月 十五 日 摘 要 茴拉西坦(aniracetam),又称阿尼西坦，化学名为1-(4-甲氧基苯甲酰基)-2-吡咯烷酮,是γ-内酰胺类脑功能改善药,临床曾主要用于治疗脑血管病后遗症。近年研究表明，茴拉西坦对老年性痴呆等有肯定的疗效,可提高患者脑内乙酰胆碱水平,有利于胆碱能神经的传递,提高学习和记忆能力[1,2]。与其传统药物吡拉西坦(脑复康)相比，具有作用强、起效快、毒性低的特点，临床上现多用于预防和治疗脑血管病、老年性记忆减退所引起的精神和行为障碍。 文献报道的茴拉西坦合成路线有多种，其中最主要的是以吡咯烷酮为起始原料，经与氢化钠或氢氧化钾反应生成钠盐或钾盐，或用氯化三甲基硅烷硅烷化后，再与对甲氧基苯甲酰氯反应获得[3～5]，但收率普遍偏低。或存在原材料价格较昂贵，难以大规模生产以及易潮解、易燃烧、毒性大、操作危险性大等问题。本文分析总结国内外文献中应用较为广泛的几种合成方法，选取其中原料易得、条件简单、易于操作者进行实验探究，以求获得其更佳合成方法。并在实验过程中适当改变实验条件，尝试以尽可能低的成本获得相同的目的。 关键词：茴拉西坦；合成；路线；原料 ABSTRACT The aniracetam,also konen as Draganon, whose chemical name is 1-(4- Methoxybenzoyl)-2- Pyrrolidone, is a γ- lactam drug of improning the brain function.It has been used to treat the sequela of the Cerebrovascular disease.In recent years, studies have shown that the aniracetam has the positive effect on Alzheimer’s disease and some other disease. It can improve the acetylcholine levels in the patienes’ brain. It’s beneficial to the conduct of cholinergic nerve and improve the ability of learning and memory. Compared with the piracetam,a traditional drug, aniracetam is more stronger, faster onset and more secure. In the clinical, it’s usually used to prevent and treat Cerebrovascular disease and the mental and behavioral inability caused by the age-related memory loss. There are many synthesis routes of aniracetam in the literature. The most important of them is using the Pyrrolidone as the raw material, then react with sodium hydroxide or potassium hydroxide. The resultant of reaction is sodium salt or potassium salt. Another route is that making the aniracetam reacting with the Methoxybenzoyl chloride after silylated by the Chlorotrimethylsilane. But the yield coefficient of this route is very low.