吡唑酰胺衍生物和杂环硫醚衍生物的合成与生物活性分析-synthesis and biological activity analysis of pyrazole amide derivatives and heterocyclic thioether derivatives.docx

j硕士茧生论文、ii盯!!、‘]l【!Sl‘摘要本论文较系统地概述了近年来吡唑衍生物和杂环硫醚衍生物在农药研究开发过程中的研究成果及研究现状。 为了寻找具有较高生物活性的吡唑酰胺衍生物和杂环硫醚衍生物，利用生物等排性原理和活性亚结构连接法设计并合成了两个系列共计38个未见报道的新型杂环化合物(见下图)，并通过IR、1H NMR、MS、Raman光谱和元素 分析对所合成的化合物进行了结构确认和表征。HT-e◇◇HET=Rq姆◇ ukH 3CH，——一N叶～N7}，耍c_＼．弋、S、H3CNN’H2NNH3CR2H，F，Cl，Br，CH3硕士学位论文^n‘r[R’H匕S!、对目标化合物的合成条件进行了探索。在实验过程中发现：在合成化合物 la-t时，用氯仿和少量的极性非质子的DMSO作溶剂，可以使反应处于均相条 件下较好地进行；在合成化合物lIa．r过程中，发现用低沸点、高极性的溶剂(如 甲醇、丙酮等)，可以较高产率的得到目标化合物。对所合成的目标化合物进行了除草、杀菌活性的初筛，生测结果表明：部 分化台物表现出良好的杀菌、除草活性(达A级)。并对化合物的结构与生物 活性的关系进行了初步的分析和讨论。关键词毗唑；毗唑酰胺；硫醚；生物活性：合成AbstractA great progress has been achieved in recent years in terms of the study of the derivatives ofpyrazole and thioether containing heterocycles，which have biological activity and carl be used as pesticides，such as，herbicides，fungicides，insecticides， acaricides．The recent studies ofthem have been reviewed in this thesis．In order to explore novel derivatives of pyrazole and thioether containing heterocycles which have higher biological activity,we designed and synthesized two series ofnew compounds according to the principle ofcombination ofbioactive substructure and bioisoteric relationship．The structures of the target compounds(1a-t and IIa·r)have been confirmed by MS，1H NMR，IR,Ranlan spectrum andelemental analysis．And their structures are as follows：HET=n0≥HR毋驭义N---。-父N(1a-t)During the courses of the synthesis of target compounds la-t，we found thm when the mixture ofehloroform and dimethylsulfoxide(DMSO)WaS used as solvem， the reactants are in the sa／rle phase SO that the reaction Can happen easily．We alsofound that when the solvents．such as acetone and methanol which have 10W boilingpoints and high polarity，are used in the synthesis of target compounds Ila．r，good yields Can be obtained．1Il肛州 一岍心 N＼一、、／S等卜 也O月__t?、’÷HETCH，cH3(IIa-r)N——N，／≮N]H1CNNH3C7 7。?1N／／。Primary bioassay showed that some of the compounds have good herbicidal and fungicidal activity．The relationship of slructure and bioactivity has been analyzc：d and discussed primarily．Ke