合成1 5 苯并硫氮杂卓及其衍生物的相关反应的研究-study on the related reactions of synthesizing 1 5 benzothiazepine and its derivatives.docx

优化工作。此项工作，为合成新型1,5-苯并硫氮杂卓衍生物的研究工作提供了实验依据。关键词：1,5-苯并硫氮杂卓抑菌活性亚胺型1,5-苯并硫氮杂卓烯胺型1,5-苯并硫氮杂卓Abstract1,5-benzothiazepineisakindofcompoundwhichhasimportantphysiologicalactivities.Someofitsderivativeshavebeenusedinclinicasantianxietydrugs,hyprosisandcardiovascularmedicines.Therefore,itssyntheses,structuresandpharmacologicalactivitieshavebeenattractedwideattentions.Experimentsprovedthat1,5–benzothiazepineareaclassofcompoundswithspecificstructures.Throughtheantibacterialactivityofthecompounds,Wehavefoundthatdifferentstructuresofthesecompoundshavedifferentphysiologicalactivity.Atpresent,theresearchgroupfortheSynthesisofresearchworkmainlyfocusedonthesynthesisof1,5-benzothiazepine-β-lactamand1,5-benzothiazepinethesetwotypesofcompounds.Wehaveanalyzedantibacterialactivityofallthevariouscompoundsthathavebeensynthesized.Itistheconsequentthatwithesterof1,5-benzo-N-imine-typeheteropolycompoundsZhuohasgoodantibacterialactivity.Ourpreliminaryviewisthatesterandiminedoublebondaretheefficacyofsuchcompounds,functionalgroups.Inordertoclarifyiminedoublebondistheefficacyofsuchcompoundsthatisonefunctionalgroup.InthispaperSelectivereductionmethodsofcontainingesteranddoublebondintheimineof1,5-benzo-N-imine-typeheteropolycompoundsZhuowerestudied.Itsantimicrobialactivityof1,5-benzothiazepinederivativeswillbeverygoodifitsmotherring2Catomsarereplacedbyester.Therefore,inthisthesislongchainα,β-unsaturatedketonessyntheticmethodsarecarriedoutrelevantresearch.Thejobprovidesanimportanttheoreticalbasisforstudingofsynthesiswithaspecialpharmacologicalactivityof1,5-benzothiazepineclassofdrugs.Themainjobsinthisthesisisasfollows:Fristly,InthispaperSelectivereductionmethodsofcontainingesteranddoublebondintheimineof1,5-benzo-N-imine-typeheteropolycompoundsZhuowerestudied.Andtheexperimentalconditionswereoptimizedforthework..Secondly,usingtheabovereductionmethod,WesuccessfullysynthesizedⅣa-eofthesefivecompounds.AndWedeterminetheirstructuresthroughthecharacterizationwork..Thirdly,Ⅳa-ethesefivecompoundsweredeterminedinv