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1、Tableofcontents65TableofcontentsDesignandsynthesisof1,1-diphenylsubstitutedbutenederivativesandtheiropeningactivitiesonBKchannelSHAYu,CHENGMao—sheng,NONOMURATaro.0HWADATomohiko70R2Fifteentargetcompoundsweredesignedbychoosingtamoxifenastheleadcompoundsandweresynthesizedbyi
2、nter—molecularMcMurrycouplingreactionandtheirstructureswerecharacter—izedbyFAB—MS,high—resolutionFAB—MSandH—NMR.Pre—liminaryassaybyusingthefluorescentdyemethodwithDiBAc4(3)wasappliedwithratrSlo12'and卢lstablyexpress—inghumanembryonickidney(HEK293)celllines.MostofthemshOWsi
3、milaractivitiesastamoxifen.Novelsemisyntheticmethodofpacli?taxelviaasymmetricaminohydroxy-lationNANPeng—juan.JIANGRu,IIUXue—ying,YAOZhi—jun,SUNXiao-1i745HOTheCl3sidechainofpaclitaxelwassynthesizedviaasymmetricaminohydroxylationoftrans—cinnamate,finally,paclitaxelwasgenera
4、tedbycondensing(4S,5R)一N—benzoyl一2一(4一methoxy)phenyl一4一phenyl一1.3一oxazolidine一5一carboxylicacidwith7一tri—ethylsilylbaccatin—llI,deprotectionandpurification.TheidentificationandsynthesisimpurityAinbudesonideCHAOJian-ping,XIAQing,RENJin-yan,WANGFu—jun,LINGYang—zhi79oftheThei
5、mpurityAinbudesonideproductwasisolatedandpurifiedanditSstructurewasconfirmedbyspectrometricanalysisvia1Dand2DNMR,ESI—MS,theimpurityAwassynthesizedinordertoconfirmthatthestructureiS16a—butanoyloxyprednisolone.BasedonthestructureoftheimpurityA,thepossiblerouteswhichwouldfor
6、mtheimpurityAwerediscussedandthepreparationprocessforbudes—onideWasimprovedtoeliminatethisimpurityA.SynthesisofN-[2.(4-trimethylacetoxybenzenesulphonamino)benzoy1]glycinebenzylesterSUNJin-rui,GUODa—liangc.NHcH:c..cH:-O+(CH3,3CCOO——≤一s.:c-一(CH3)3CCOO'-@∞HcH2C00cH2Thekeyint
7、ermediateofsivelestatsodium,N一[2一(4一trimethyl—acetoxybenzenesulphonamino)benzoy1]glycinebenzylesterwassimplysynthesizedbythecondensationoftrimethylacetoxy—benzenesulfonicchlorideandN—f2一aminobenzoy1)glycinebenzylalcoholester.Therawmaterialsinthisrouteischeap,andthereactio
8、nconditioniSeasytOcontrolwithhigheryield.L?≯lTableofcontents82Synthesisof(2S.4S)-4-acetylthio-1-