ⅳ抑制剂vildagliptin及其类似物的合成分析

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1、优秀毕业论文用机制，保留1一(2一氯乙酞基卜2一(S)一氰基毗咯烷，引入了呱嚓环和酞胺键。并在此基础上对化合物进行结构修饰，主要从改变芳香基团上的取代基上进行。芳香基团上的取代基的种类有甲氧基、氯、甲基、硝基等，从而合成了一系列具有不同呱嗦侧链结构的维达格列汀类似物。5.以呱嗦为原料，以冰醋酸为溶剂，对呱嗦进行单酞化反应，通过注意控制反应条件，确保单酞基呱嗦产物的产率，降低双酞基呱嗓的产生，而后单酞基呱嗦与1一(2一氯乙酞基卜2一(S)一氰基毗咯烷发生取代反应得目标化合物。其中目标化合物五个，均未见文献报道，其结构经lR、’H

2、NMR和Esl一Ms进行了确证。由于硕士论文时间较短(学制两年半)进一步的药理实验正在进行之中。关键词:糖尿病治疗药;DPP一W抑制剂;维达格列汀;合成工艺;结构修饰精品参考文献资料优秀毕业论文StudiesonthesynthesisofVildagliPtinanditsanologuesasdiPePtidylPePtidaseIVinhibitorsABSTRACTRecently，thePrevaleneeofdiabetieshasinereaseddramatieallyandbeeometothethirdde

3、athfaetorinferiortoeardiovaseulardiseaseandtllmor.SomenewantidiabetiedrugswithhighefficieneyandlowtoxicityweredevelopedforclinicaPPlieationduringthePastfewyear、.DPP一IVinhibitorsasanewkindofantidiabetiedrugshaveattraetedanextensiVeattentioninrecentyears，andVildagliPt

4、in15therePresentativedrugofDPP一IVinhibitorsinelinie.ThisartielesummarizedtheresearehProgressesontheantidiabetiedrugs，esPeciallyonthesynthesisofDPP一IVinhibitorsfirstlyandthenaPratiealSynthesisforVildagliPtinwasdeveloPedbytwosynthetieroutes.AceordingtotheSARforVildagl

5、iPtinanalogues，fivenoveleomPoundsweredesignedandsynthesized.ThemaineontentsofthisPaPerareasfollws:1.3一amino小adamantanol15animPortaniintermediateinthissyntheticroute.AftereomParingtheroutesinliteratures，thissynthetieroutewasehosedandimProvedas:1一adamantylamine·HCIass

6、tartingmaterial，afternitrated，treatedbyalkalitogivetheimportantintermediatel一Aminoadamantane一3一01with72%yield.ft15suitableforlarge一sealePreParation.2.InthisPaper，l一(2一ehloroaeetyl)一2一(S)一eyanoPyrrolidinewassynthesizedbytwodifferentroutes.Routeoneinvolvesthereaetiono

7、ftheL一Prolinewastreatedbyammoniafirst，thenreaetedwithaslightmolarexeessofchloroaeetylehloridetogivel一(2一ehloroaeetyl)一2一(S)一Pyrrolidinamide.Andthenl一(2一ehloroaeetyl)一2一(S)一cyanoPyrrolidinewassynthesizedbydehydrationinthePreseneeoftrifluoroaeetieaeid.Routetwo15touseL

8、一Prolineasstartingmaterial.L一ProlinewasN一aeylatedwithehloroaeetylehloridetoaffordl一(2一chloroacetyl)Pyrrolidine一2一(S)一earboxylicaeid，thentr