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1、AbstractIntheseventiesoflastcentury,theChinesediscoveredgossypolcallbeusedasanonsteroidalmaleoralcontraceptivefirstly,whichraisedseriesofstudiesofgossypolintheinternational．However,afterlong-termmedication,gossypolshowestwounavoidablesideeffects，hypokal
2、emiaandirreversibilityoffertility,whichgreatlylimitstheclinicaluseofgossyp01．Gossypolnotonlyhassignificantanti—fertilityofmalerole，butalsohasa丽derangeofapplicationsinthegynecologicalclinic．InMdition,gossypolalsohasstronganti-tumor,anti-viralandimmuneinh
3、ibition．Inordertomakebetteruseofgossypol，chemistshavedesignedandsynthesizedaseriesofgossypolderivatives，whichhavetheeffectofgossypolbutlowtoxicity．Thebiologicalfunctionofgossypol，thedesign,synthesisandapplicationofgossypolderivativesweremainlystudiedint
4、hispaper．Throughliteraturereview,wedesignedthesynthesisrouteof5-benzoyl·1，4一naphthoquinoneandstudiedthesynthesistechnologycarefully．Withmalomcacidandaeroleinasstartingmaterials，thekeyintermediate5,8一dimethoxy—naphthoicacidcanbepreparedinafive—stepproced
5、urewhicharecondensation,Diers-Aldercyclization,methylation,aromatizationandhydrolysis．Finally,5-benzoyl-l，4一naphthoquinoneCanbeobtainedbyFriedel—Craftsacylationandoxidationofthekeyintermediate．Asyntheticproeedurewithmildreactiveconditionsandcheaperstart
6、ingreagentsfor5-benzoyl-1，4-naphthoquinoneisachieved，whichissuitableforlarge—scalepreparation．Asisknowntoall，1,4-naphthoquinonecompoundshavesignificantanti-tumoreffect．Basedontheanalysisofstructure-activityrelatiomhip(SAR)of1,4-naphthoquinone，differentt
7、ypesof5-substituted1,4-naphthoquinonecompoundsweredesignedandprepared，whichwereconfirmedbyⅡ乙1H-NMRandMS，allofthemarenewcompounds．Inaddition,theanti-tumoractivityandantifertilityacti、ri锣ofthenewcompoundswillbetestedinvitro．Throughanalysisoftestresults，th
8、eanti-tumormechanismof1,4-naphthoquinonecompoundsanddifferenttypeSof5-substituenteffectsonitsactivitywillbestudiedfuthermore．Keywords：gossypol，naphthoquinone，anti-tumor，antifertility，synthesis-Ⅱ-第一章棉酚类似物的研究进展1．1．棉酚的结构、物化性质以及提取方法1
