生物活性黃酮槲皮素的前藥設(shè)計(jì)與合成研究.pdf

1、四川大學(xué)碩士學(xué)位論文生物活性黃酮槲皮素的前藥設(shè)計(jì)與合成研究姓名：伍賢學(xué)申請學(xué)位級(jí)別：碩士專業(yè)：有機(jī)化學(xué)指導(dǎo)教師：成麗20050515生物活性黃酮槲皮素的前藥設(shè)計(jì)與合成研究StudiesOUprodrugdesignandsynthesisofbioactiveflavonoidquercetinSpecialty：OrganicChemistwGraduateStudent：Xian—xueWuSupervisor：LiChengQue

2、reetinisakindofflavonoid，whichiswidelydistributed，inmanydietaryandmedicinalplantsincludingonion，apple，tea，ginkgobilobaandothersItisas訂ongnaturalantioxidantandsohavelotsofimportantpharmacologicalactivities，suchaspreventio

3、nofcardiovasculardiseases，anticancerandneurodegenerativeinhibitionVoluminousanimalstudiesandlimitedhumanstudiesshoWthatitiSthebadsolubilityinpharmaceuticallyacceptablesolventsandbadpharmacokineticpropertiesthatleadtothep

4、oorabsorption／availabilityafteroraladministrationofquercetinandSObadlyaffectedtheclinicdevelopmentofquercetinThereforeitissignificanttodesignandsynthesizequereetinderivatives、Ⅳithenhancedwatersolubilityandbetterpharmacok

5、ineticpropertiesbystructuremodificationonquercetinItisapityfewstudiesonthisworkwerefoundintheliteratureSOfarDuringourworkaimedatsynthesisofquercetinderivativesusedaspotentialprodrugordrugcandidates，aseriesofaminoacidcarb

6、amatesofquercetinweredesignedandsynthesizedfiomcommerciallyavailablequercetinandendogeneticL—aminoacidutilizingtriphosgene(BTC)asanauxiliaryreagentFirstlytwostrategiesforconstructionofquercetincarbamateswerecomparatively

7、researchedtogiveaberetoneasfinalchoiceTheresultshownthatitwasdifficulttogetchloroformateofquercetinbyreactionwithBTCandisocyanatecancouplewithquemetineasilySothepreferentialstrategytosynthesizequercetincarbamatewiththehe