碘代三氮唑的合成及應(yīng)用

1、STUDIESONTHESYNTHESISANDAPPLICATIONOFIODO1，2，3TRIAZOLE彳DissertationSubmittedtotheGraduateSchoolofHenanNormalUniversityinPartialFulfillmentoftheRequirementsfortheDegreeofMasterofScienceByXincuiFQnSupervisor：AssociateProfL

2、ingjunLiMay2014ABSTRACT1，2，3triazolesareimportantstructuralmoietiesindrugsynthesis，bioconjunction，andmaterialsscience，benefitingfromtheireaseofsynthesisandchemicalstabilityThecopper(I)一catalyzedazidealkynecycloaddition(C

3、uAAC)isareliablemeansforthesynthesisof1，4disubstituted1，2，3triazolesThegeneralandregioselectivesyntheticmethodologytothe1，5regioisomers，bycontrast，arenotwelldevelopedOntheotherhand，wateristhesolventofchoicefornatureinall

4、biosyntheticroutes，whichhastheadvantageofbeingabundantlyavailable，nontoxic，nonflammableandinexpensive，Withwaterassolvent(in／onwater)，remarkablereactivityandselectivitycouldalsobeachievedduetospecialsolvationandmoleculara

5、ssemblymodesInthiscontext，reactionsin／onwaterhaveattractedgreatinterestindrugdesign，materialsscience，andbiologicalprocessesTherefore，basedonourpreviouswork，thisdissertationhascardedoutthemethodologiesresearchofmultisubst

6、itutedand1，5disubstituted1，2，3triazolesTheinnovationsinclude：(1)multicomponentsynthesisof5iodo1，2，3triazolesinthepurewatermedium(2)synthesisofthedualfunctional4TMS5iodo1，2，3triazoles，followingthedevelopmentofanewmethodol

7、ogytosynthesize1，5一disubstituted1，2，3triazolesand1，4，5trisubstituted1，2，3triazolesThedetailsareshownasfollow：1Reviewofthedevelopmentofiodinationanditsapplicationinthefieldofbio—labeling，drugsynthesis；reviewthelatestprogr

8、essonsynthesismethodologyof1，4，5disubstituted1，2，3triazolesandit’Sapplicationindrugdesign2Developedanewmethodofthesynthesisof5iodo一1，2，3triazolesinthepresenceofCuI／selectflulor／DIPEAinwaterwithteminalalkyne，azideandtetra

9、butylammoniumiodideasstartingmaterialsThehightoleranceofvarioussensitivegroupsandhighchemoselectivityrevealedthepotentialofthismethodinorganicsynthesisanddrugdiscovery3Developedanewrouteofthesynthesisof5aryloxy一1，2，3tria