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1、毕业论文题目中枢兴奋药茴拉西坦的合成研究-21-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
2、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-21-ABSTRACTTheaniracetam,alsokonenasDraga
3、non,whosechemicalnameis1-(4-Methoxybenzoyl)-2-Pyrrolidone,isaγ-lactamdrugofimproningthebrainfunction.IthasbeenusedtotreatthesequelaoftheCerebrovasculardisease.Inrecentyears,studieshaveshownthattheaniracetamhasthepositiveeffectonAlzheimer’sdiseaseandsomeotherdisease.Itca
4、nimprovetheacetylcholinelevelsinthepatienes’brain.It’sbeneficialtotheconductofcholinergicnerveandimprovetheabilityoflearningandmemory.Comparedwiththepiracetam,atraditionaldrug,aniracetamismorestronger,fasteronsetandmoresecure.Intheclinical,it’susuallyusedtopreventandtre
5、atCerebrovasculardiseaseandthementalandbehavioralinabilitycausedbytheage-relatedmemoryloss.Therearemanysynthesisroutesofaniracetamintheliterature.ThemostimportantofthemisusingthePyrrolidoneastherawmaterial,thenreactwithsodiumhydroxideorpotassiumhydroxide.Theresultantofr
6、eactionissodiumsaltorpotassiumsalt.AnotherrouteisthatmakingtheaniracetamreactingwiththeMethoxybenzoylchlorideaftersilylatedbytheChlorotrimethylsilane.Buttheyieldcoefficientofthisrouteisverylow.Therearealsosomeotherroutes.However,thisrouteshavetheshortcomingslikethatther
7、awmaterialistooexpensivetobeusedtolarge-scaleproduction,beingdeliquescent,easytoburn,withhightoxicityandoperatingdangerousandsoon.Inthisarticle,weanalyzeandsummarizesomesynthesismethodswhichwerewidelyusedinthedomesticandforeignliteratureworksandselectsomeofthemwhoserawm
8、aterialiseasygetting，reactionrequirementsaresimpleandeasytoconducttodoexperimentinvestigationswiththepurposeof
