含吲哚结构螺环化合物合成的研究.pdf

含吲哚结构的螺环化合物的合成研究摘要摘要多组分反应因其所具有的连续,高效,操作简便,反应收率高等优点,在近年来受到了学术界的普遍重视和广泛关注。多组分反应可以快速有效地构建大量具有结构复杂性和多样性的化合物以便从中寻找具有重要生理和药理活性的药物前驱体,因而已经成为了有机化学和药物化学工作者手中不可或缺的重要工具。与此同时,吲哚衍生物也因为其重要的生理及药理活性,同样成为了人们关注的热点。本论文主要研究了利用多组分反应,构建含吲哚基团的螺环化合物的方法, 主要分为以下rL个部分。第一部分研究了利用靛红,,,在水相中一锅法合成了一系列新型的吲哚螺环衍生物。这种方法具有高效、反应条件温和、操作简单以及环境友好等优点。、靛红、巯基乙酸的多组分反应,三组分一锅法高效合成了吲哚螺吡唑并[3,4一el[1,41硫氮杂卓衍生物。该合成方法具有产率高、底物范围广泛、反应条件温和以及反应处理简单等特点。第三部分主要研究了邻苯二甲酰肼,靛红,丙二腈(或氰乙酸酯)的三组分反应,成功地构建了一系列新颖的吲哚螺毗哗并【l,】酞嗪衍生物,该合成方法高效、反应条件温和、一锅法,且操作简单。关键词:吲哚,靛红,螺环化合物,多组分反应,一锅法合成。作者:陈辉指导教师:史达清教授 Study on theSynthesis ofIndole—-Containing pounds Abstract ponent reactions(MCRs)have attractedincreasing attentionby virtueof theirconvergence,productivity,ease ofexecution andgenerally highyields ofproducts· As aresult,it e apowerful enerating librariesofmolecules forthe discovery andstructuraloptimizmion ofbiologically activeleadsandpotentialdrug addition,indole derivatives have long been thefocusofconsiderable attention due totheirabundant existence innumerous nature products aswell astheir extensiveapplications inbiological andpharmacological area. In this dissertation,our attention mainly focuses on the construction of pounds viaone-pot ponent reactions. Part I:An efficient and of novel spirooxindole derivatives via ponent reaction of isatin,5- and 1,pounds inaqueous medium advantages ofthis method include highefficiency,mild reactionconditions,convenient operation,and environmentally benign conditions. PartII:An synthesis ofspiro[indoline-3,4’-pyrazolo[3,4。P】【l,4】 thiazepine]dione ponent reactionof5-amino-3一methylpyrazole, isatin,and ,valuable featuresofthismethod include thegood yields oftheproducts,broader substratescope,mild reactionconditions,and convenient operation and thestraightforwardness oftheprocedure. Part III:A facile and efficiententry intospir