1，5-苯并硫氮雜卓-β-內酰胺衍生物的合成與研究.pdf

1、河北師范大學碩士學位論文1，5苯并硫氮雜卓β內酰胺衍生物的合成與研究姓名：付江霞申請學位級別：碩士專業(yè)：有機化學指導教師：李媛張萍20050520——一一竺!!塑AbstractI，5benzothiazepineisakindofcompoundwhichhasimportantphysiologicalactivitiesSomeofhisderivativeshavebeenusedinclinicasantianxietydru

2、g，hyprosisandcardiovascularmedicineThereforehissynthesess咖ctmosandpharmacologlcalactivitieshaveattractedwideattentionsTheC=NdoublebDndinthemoleculesCanmodifythebenzothiazepinewhichisoneofthemajorpartswherechemicalreactio

3、nsoccurredThusaseriesofnew15一benzothiazepinederivativeshavebeensynthesizedanddevelopedOurgrouphavebeendoingextensivestudiesontheir【22】cycloadditionreactionsInthisthesis，wehaveobtainedaseriesofnewB—tactarnderivativeofthe1

4、，5benzothiazepinethroughthereactionofthepotassiumsaltofmalicmidewhichisactivatedbyC1COOEtandthe1，5benzothiazepineThespectrumwasanalyzedandstudiedOurworkisimportanttofindtheirspecialfunctionsandnewactivechemicalcompoundso

5、fphysiology1Startfrom(DL)一malicacid，thenfollowthenextfourreactionsteps，suchasesterification，carboxylprotection，wegbtthemalicanhydridewhichisusedasthe瑚H2protectionagentofaminoacidreactedwithaminoacidThroughthisreaction，we

6、getmalicmideaceticacidanddevelopitssixreactionconditionsWealsofinditsoptimumreactionconditions2，F(xiàn)irstlyweletthepotassiumsaltofmalicmideprotectedwithcarhoxylreactwiththeCICOOEtwhichisusedastheactivatorinthisreactionSecond

7、lywelettheproductionreactwiththeC=NofthebenzothiazepineunderthesurroundingofEt3Nsolution，SOweobtainaseriesofuewB—lactamderivativesofthe15一benzothiazepinThestructuresoftheproductionaredeterminedbyIR、1HNMR、MSandelementarya

8、nalysis3Wesubstitute(DL)一malicacidfor(S)macidacidandsynthesizethemalicanhydrideprotectedwithcarboxylwhichhastheopticpropertiesWegoonthesamestepsastheabove，thatisletthemalicanhydridereactwith15benzothiazepintogettheBlaeta