含吡唑类化合物合成及生物活性地研究.pdf

青岛科技火学研究生学位论文含吡唑类衍生物的合成及生物活性研究摘要近年来,多种毗唑类衍生物具有良好的生物活性,倒如杀虫、杀蔺承f『绘毕等。另外,一些含呲唑的稠杂环衍生物也表现出较高的农药活性。为了寻找具有更高生物活性的吡畔类先导化合物,在查阅文献的基础上,设计合成了5个系=歹d45个新型的毗呻类衍生物。并初步测试了其尘物活性。结果袭i妣部分化合物具有杀菌、除草、植物生长调节活性。本论文以卜取代-5-甲基毗唑酰肼为创制源,将其分别与2一氰基一3,3一二甲硫基丙烯腈、2一氰基一3,3-'-"甲硫基丙烯酸乙酯、乙氧次甲基丙二腈、乙氧次}f『基氰基丙烯酸乙酯、N一氰基亚氨二硫代碳酸二甲酯(CIDT)等合成子反应,得到了新型的吡唑羰基吡唑、吡唑羰基三唑化合物(1—5)。与苯基异硫氰般雌反应得到吡唑氨基硫脲类化合物,在酸性、碱性、碘/碘化钾条件下得到吡畔连杂qi(6) 类化合物。将呲唑酸与三唑、毗唑连三唑与各种取代苯甲酸反应,得到含吡IJ牛基的稠杂环(7、8)类化合物。曹《:逸岬呲。, 龠删HNHcS洲囝 CH3 6 镶飘含吡唑类化含物的合成及生物滔性研究. H 所合成的化合物的结构均经1H NMR、IR、元素分析确证,部分化合物的结构通过MS、X-ray单晶衍射进一步确认。关键词:吡唑,吡唑连杂环,合成,生物活性,光谱性质,反应机理,晶体结构青岛科技火学研究生学位论文 STUDIES ON THE SYNTⅡESIS AND BIOLOGICAL ACTIVITY oFNEW SUBSTITUTED PYRAZOLYL DERIVATIVES Abstract recent years,many pyrazole derivatives have shown high biological activities,such as insecticide,fungicide and herbicide,etc Moreover,some fused pyrazole derivatives have also exhibited high biological activities search of novel pound containingpyrazole derivativeswithhigher potential biological activities 5series,45 new pyrazole derivatives were synthesized,The biological activities pounds were examined and theresultsshowed that some ofthem had fungicidal,herbicidal or plant-grownth regulating activities, Inthispaper,by reactions ofl-substituted一5哪!ethylpyrazolhydra‘ zine with 2-cyano一3,3一dimethyl thioacrylonitrile,2-cyano一3,3一dimethyl— thioacrylate,ethyloxymethylenemalononitrile,2-cyano-3一ethyloxyacryl— ateN-Cyanoimido-S,S—dimethyIdithiocarbonate,we synthesized 3series of new pounds(1-5),with phenyl isothioeyanates afford the thiosemicarbazides,which were converted 含毗l业类化合物的合成及生物活性研究 intopyrazole—heterocyclic(pounds inKI/12,base and acidsolution pounds(7,8)were synthesized by reaction of 3-subtituted-4-amino一5一mercapto一1,2,4一triazoles with pyrazole acid R R o c\N—N ,H,Nb八sM。 CN(C00Etl O o N(C00Et) NHNHCSN 6 H R The structures ofthese 5series,45 pounds were confirmed by 1HNMR,1R,elemental analysis and ,two crystal structures pounds were studied