Table of contents

1、Table of contents65TableofcontentsDesignandsynthesisof1,1-diphenylsubstitutedbutenederivativesandtheiropeningactivitiesonBKchannelSHAYu,CHENGMaosheng,NONOMURATaro.0HWADATomohiko70R2FifteentargetcompoundsweredesignedbychoosingtamoxifenastheleadcompoundsandweresynthesizedbyintermolecularMcMurrycouplin

2、greactionandtheirstructureswerecharacterizedbyFABMS,highresolutionFABMSandHNMR.PreliminaryassaybyusingthefluorescentdyemethodwithDiBAc4(3)wasappliedwithratrSlo12and盧lstablyexpressinghumanembryonickidney(HEK293)celllines.MostofthemshOWsimilaractivitiesastamoxifen.Novelsemisyntheticmethodofpacli?taxel

3、viaasymmetricaminohydroxy-lationNANPengjuan.JIANGRu,IIUXueying,YAOZhijun,SUNXiao-1i745HOTheCl3sidechainofpaclitaxelwassynthesizedviaasymmetricaminohydroxylationoftranscinnamate,finally,paclitaxelwasgeneratedbycondensing(4S,5R)一Nbenzoyl一2一(4一methoxy)phenyl一4一phenyl一1.3一oxazolidine一5一carboxylicacidwit

4、h7一triethylsilylbaccatinllI,deprotectionandpurification.TheidentificationandsynthesisimpurityAinbudesonideCHAOJian-ping,XIAQing,RENJin-yan,WANGFujun,LINGYangzhi79oftheTheimpurityAinbudesonideproductwasisolatedandpurifiedanditSstructurewasconfirmedbyspectrometricanalysisvia1Dand2DNMR,ESIMS,theimpurit

5、yAwassynthesizedinordertoconfirmthatthestructureiS16abutanoyloxyprednisolone.BasedonthestructureoftheimpurityA,thepossiblerouteswhichwouldformtheimpurityAwerediscussedandthepreparationprocessforbudesonideWasimprovedtoeliminatethisimpurityA.SynthesisofN-2.(4-trimethylacetoxybenzenesulphonamino)benzoy

6、1glycinebenzylesterSUNJin-rui,GUODaliangc.NHcH:c.cH:-O+(CH3,3CCOO一s.:c-一(CH3)3CCOO-HcH2C00cH2Thekeyintermediateofsivelestatsodium,N一2一(4一trimethylacetoxybenzenesulphonamino)benzoy1glycinebenzylesterwassimplysynthesizedbythecondensationoftrimethylacetoxybenzenesulfonicchlorideandNf2一aminobenzoy1)glyc

7、inebenzylalcoholester.Therawmaterialsinthisrouteischeap,andthereactionconditioniSeasytOcontrolwithhigheryield.L?lTableofcontents82Synthesisof(2S.4S)-4-acetylthio-1-(4-nitrobenzyloxycarbony1)-2-(3-anyl-oxycarbonylphenylcarbamoy1)pyrroli-dineZHONGZhao-jin,WUYah-bin,LIUJunH0HH3COS-0O.一Tosynthesizeakeyi

8、ntermediateofertapenem.(2S,4S)一4一acetylthio一1一(4一nitrobenzyloxycarbony1)一2一(3一allyloxycarbonylphenylcarbamoy1)pyrrolidinewasefficientlysynthesizedfromreadilyavailabletrans-4-hydroxy-L-prolineviasixstepreac-tions.Theoverallyieldis49.4%.Theprocessisconvenientandsimpleforpharmaceuticalmanufacture.Synth

9、esisoflanoconazoleLIChujun,SHENGJJanwei,RENYi.GUOChun91.HC00HLanoconazolewassynthesizedfrom2一chloromandelicacidthroughanimprovedprocesswiththeadvantagesofeasyoperation,lowcostandbeingsuitableforindustrialproduction.Thetotalyieldis2O.4%.SynthesisofcefozopranhydrochlorideYUTao.ZHANGKeliang,WANGHui,ZHA

10、OYanfang,GONGPingC00H0CHTheintermediate7一amino一3一(3一imidazo1,2-bpyridazin一4一ium一1一y1)methy1一3一cephem一4一carboxylicacidhydrochloridewassynthesizedfrom7一ACAbyprotection,substitution,andcondensationwithbenzothiazolylthiolactiveestertoobtainthefourth-generationcephalosporincefozopranhydrochloride.Thetota

11、lyieldiS12.9%from7一ACA.-4?-r啦C93TableofcontentsBioactivealkaloidsandsterolsfromaAmarinefungus96F197wasisolatedbysilicagel,ODScolumnmarinefungus96F197chromatography,sizeexclusioncolumnchromatography(SephadexIH一20),andreversedphaseHPICpurification.SONGShanshan,WANGNaili,StructuraIelucidationwasachieve

12、dbyphysicchemica1con-GAOHao,LIUHongwei,stantsandspectroscopicanalysis.MTTwasusedtoevaluatetheZHANGOing-hua,MICHIONamikoshi,bioactivities以,1D.Twoalka1oidsandtwostero1swereisolatYAOXinshengedfromacetoneextractsofmvceliumofstrain96F197andelucidatedasviridicatol(1),sclerotiamide(2),22E一5a,6aepoxyergosta

13、-8(14),22一diene一3口,7adiol(3),22E一5a,8aepidioxyergosta-6,22一dien一3j9一ol(4).Coumpoud3and4canevidentlyinhibitthegrowthofcancercellsHepG2.MCF一7andNCIH460attheconcertrationof50/*g.mL_.Compound3and4showanticancerbioactivitiesinvitro.98Theconstituentsofmarinefungus97F49ZHANGQinghua,WANGNaili,GAOHao,LIUHong

14、wei,SONGShan-shan,MICHIONamikoshi,YAOXinsheng102Thebrothof97F49wasisolatedbysilicagel,SephadexLH一20,ODSandRPHPLCchromatographies,andtheirstructureswereidentifiedbyspectralmethods+Sixcompoundswereisolated.andtheirstructuresweredeterminedas4Z一8一hydroxy一4一methyl-4一nonen一3一one(I),22Eergosta一5,7,22trien一

15、3一ol(1I),22E一5a,8a.epidioxyergosta一6.22一dien一3flol(),22Eergosta-7,22一dien一3fl,5fl,6fltriol(1V),arabitol(V),manitol().Compound(I)isanovelcompound.Isolationandidentificationofpheno-liccompoundsfromMorusmacrouraMiq.DAIShengjun,YUDequan,LOZiming,CHENRuoyun106SevenphenoliccompoundswereisolatedbySephadexI

16、H一20.RpC18,RpC8andsilicagelcolumnchromatography.TheirchemicalstructureswereelucidatedandidentifiedasmoracinM(1),2一(3,5一dihydroxypheny1)一5,6一dihydr0xybenzofuran(2),mulberrosideC(3),oxyresveratrol(4),3,5,2,4-tetrahydroxy-4一(3一methyl一1一buteny1)stilbene(5),mulberrofuranG(6),mulberrofuranK(7).Forthefirst

17、time,compounds17areobtainedfromthisplantwhilecompounds3and5areisolatedfromMorus.ImprovedsynthesisofliranafateUWei,CHANGXuanniu,HAOErjun,HEXinlei=)+d_J午H.CH36一Methoxy一2一(methylamino)pyridinewassynthesizedfrom2,6一dichloropyridine.5,6,7,8一tetrahydro一2一naphthylthiochloroformatewassynthesizedfrom5,6,7,8一

18、tetrahydro一2一naphtho1.Liranafatewasobtainedbythereactionof6一methoxy一2一(methylamino)pyridineand5,6,7,8tetrahydro一2一naphthylthiochloroformateinthepresenceofK2CO3.5Tableofcontents108.SynthesisofaripiprazoleZHUHangchang,CHENGuo-hua,H3CZHANGJun-ren,LIQiang110Aripiprazolewassynthesizedfromm.anisidineviaco

19、ndensa.tion,FCacylation,etherfication,substitution.Thetotalyieldis45.1%.Improvedsynthesisof2-cyanopyrimi-dineCAIWeibing,CHENYubinH,)3Cr一NjL,cNN2Cyanopyrimideissynthesizedfrom2一(trimethylammonio)一pyrimidinechlorideandpotassiumcyanide,inthesolutionofammoniumchloride,vianucleophilicsubstitution.Thispro

20、cedurehasadvantageofconvenientoperationsandmildreaction.Theyieldishigherthanthatreported.112ImprovedsynthesisofcarlporideJINNing,XUYungen,HUAWeiyill4OHH3N.y,NH2lONH,Cariporidewassynthesizedfrom4一isopropylbenzoicacid.4一isopropylhenzoicacidwastreatedwithchlorosulfonicacidtoforrncorrespondingchlorsulfo

21、nylderivativewhichwasreducedbysodiumsulfite,followedbymethylationwithdimethylsulfatetogivecorrespondingmethylbenzoate.Theesterwastreatedwithguanidinetogivethetargetcompound.TheoverallyieldoftheimprovedprocedureiS45.3%.Progressontheinhibitorsofacid-Acid-sensingionchannels(AISCs),whichareactivatedbyex

22、sensingionchannelstracelluarH.areH一gatedcationchannels.ThesixsubunitsCUILin,YANGRifang,ZHENGJianquan,MARun-yu,YUNIiuhong122ofASICsfamilyhavebeenclonedandtheyplayimportantrolesinsensoryperception,suchastouch,pain,sourtaste,learningandmomoryaswellassomepathologicalconditions.ASICscanbemodulatedbyneuropeptide,tempera