咪唑立宾的合成工艺研究

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1、工程硕士论文AbstractMizoribine(Bredinin，MZR)，wasisolatedin1974fromtheculturefiltrateofEupenicilliumbrefeldianumanditsstructurewasdeterminedas4-carbamoyl一1-p-D-ribofuranosylimidazolium-5-olatebyX-raycrystallograghicanalysisanditisasyntheticpurinenucleosideinhibitor，Cansele

2、ctivelyinhibittherapidgrowthoflymphocytes，suchasTcells，Bcelldivisionandproliferation，resultinginimmunosuppressiveeffects．Inrecentyears，isusedinclinicalrejectionofrenaltransplantationrejection，butalsoforthetreatmentoflupusnephritis，nephroticsyndrome，rheumatoidarthrit

3、isandautoimmunediseases．SynthetictechnologyofMizoribineisstudiedinthispaper．Lessreportingonthedomesticsyntheticresearchmethods，inacomprehensiveanalysisofeachreportedintheliteratureabroadsyntheticroute，basedonthechoiceofDiethylaminomalonatehydrochlorideasrawmaterial，

4、bycyclizationreactiontobethekeyintermediate5-Hydroxy·-1H·-imidazole·-4·-carboxamide(SM·-108)。IntermediateSM-108ontheprotectionofhydroxylandaminosilanes，throughaiderthecondensationwith1,2，3，5一tetraacetyl-beta-D-ribofuranosetoget4-Carbamoyl一1一(2，3，5，一tri·O—acetyl·p·D—

5、ribofuranosyl)imidazolium-5-olate，andthenoutthroughthehydrolysisofacetylreceivedmizoribine．Thetotalyieldwas13％(basedonDiethylaminomalonatehydrochloride)．Throughresearch，towhichmulti-stepreactionhasbeenimprovedmethodismorepracticalthanreportedintheliterature，economic

6、，andmoreconducivetomassproduction．ThestructureofMizoribinewasconfirmedbytheapplicationofelementanalys，1H-NMR，13C-NMRandMSspectra．ThepurityofMizoribineis99．96％byHPLC．Keywords：Mizoribine；immunosuppressiveagent；kidneytransplantation；synthesis．II工程硕士论文目录摘要⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯

7、⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯VIABSTRACT⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯·VI第1章绪论⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯·11．1免疫抑制剂的发展历史01J⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯11．2免疫抑制剂的分类⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯21．2．1按作用机理分‘2】⋯⋯⋯

8、⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯·21．2．2按其来源分‘3】⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯·51．3理想免疫抑制剂‘4l⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯”6第2章咪唑立宾简介⋯⋯