1、浙江大學碩士學位論文N正丁基苯并異噻唑酮的合成研究姓名:王凌申請學位級別:碩士專業(yè):應用化學指導教師:胡望明20060501浙江大學磷士學位論文ABS薯RACTTransdermaIdeliverysystemisakindofdrugdeliverysystemthatdrugs,whichpenetratetheskinsabsorbedbycapillaryvesseIenterintothebodycirculationandb
2、ringIntocurativeeffect1nordertoovercometheskinbarrierpenetrationenhancersareoftenusedtoincreasetheblooddrugconcentrationsothattheskinpenetrationvelocityandconcentrationofthedrugscanreachthecurativedemandTherefore,thedeve
3、lopmentandapplicationofpenetrationenhancerbecomeextremelyimportantThisthesisjsaboutthesynthesisofanewpenetrationenhancerofgreatefficiency:thiazoneOrthogonaltestmethodwasusedforstudyingonthesynthesisofthiazoneunderphasetr
4、ansfercatalysiscondition,usingsodiumsaccharinand1butyIbromideasreactantstetrabutvIammOniumbromide(TBAB)asphasetransfercatalyst。Themainfac幻rsandtheminortactorswerediscussedthroughtheexperimentsTheexperimentaIresultsindica
5、tedthattherea&iontemperatureandthedosageof1_butylbromidewerethemainfactorswhilethereactiontimeandthedosageofTBABweretheminorfactorsTheincreaseofreactiontemperatureanddosageof1butylbromidecouldbothincreasetheyieldofproduc
6、tincertainscopebuttheexcessincreasingofthemmightbringinmuchbyproductsExtendingthereactiontimecouldnotremarkablyincreasetheyieldofproductWhenthemolarratioofTBABand1出utyIbromidewasabove005:thelncreaseofT8ABdosagecouldhardl
7、yincreasetheyieldTheoptimizedparameterswerethatthefeedingofsodiumsaccharinand1由utyIbromidewasonthetheoryratioat100℃for10hundertheconditionthatthemolarratioofTBABand1一butylbromidewas005:1Thustheyieldwas8763%withwhitedrysh
8、eetcrystalobtainedAnewsynthesistechniqueofthiazonewasdevelopedThefeedingofsodiumsaccharinand1butyIbromidewasonthetheoryratiointhesolventofOMFwithoutanyphasetransfercatalystTheexperimentalresultslndicatedthattheyieldofpro
9、ductincreasedatfirstbutdecreasedafterwardswhenincreasingthereactiontemperaturefoftheexcesslncreasingoftemperaturebroughtinthebyproductsjncreaseThemostappropriatetemperaturewas100℃ThemeltingpointdeterminationthelRspectrum
10、analysisandtheelementanalysisofthiazonewerecarriedoutTheresultsmatchtheIiteraturevaluesandthetheoryvaluesBesidesthese,theside。reactionandtheseparationofimpuritywerediscussedinthethesissupportingthefurtherresearchinthefut