新型炔酚类天然产物selaginelin+l的合成与结构修饰

《新型炔酚类天然产物selaginelin+l的合成与结构修饰》由会员上传分享，免费在线阅读，更多相关内容在学术论文-天天文库。

1、硕士学位论文英文摘要，ABSTRACTSofar,thescreenedmGl训飚antagonistsweredesignedeitheronthebasisoftheCADD(AidedDrugDesign)orfromthecompoundlibrarydirectly．Un6lnow,therewasnoreportconcerningthemGluR5antagonistfromthenaturalproducts．Selaginellin,whichhasanewcarbonscaffold，wasfirstisolatedfr

2、omtheSelaginellasinensisin2007byZhangLi-pingeta1．(LanZhouUniversity)．Afterwards，ourresearchgrouphassuccessfullyisolatedaserialof12derivativesofSelaginellin．AccordingtoprophasebioactivityexperimentwithSelaginellin，andanalysisoftherelatedreference，wespeculatedtheSelaginellin

3、LperhapsisthenaturalantagonistofmGluR5．·。Inthisstudy,itisthefirsttimetotakethenaturalproduct．SelaginellinLastheleadcompoundtodesignandsynthesizethemGluR5antagonist．Throughthechemicalreactions：Bromination，Suzuki，SonogashiraandDiazotization，etc．，wesuccessfullysynthesizedthet

4、argetcompounds一-ND一·selaginellin13andN口EPa9．Thestructureswereconfirmedbythemodemspectrumtechnology．Inaddition，thisstudyexploredthesynthesisroutesoftllerelatedcompounds．Wedesignedthreesynthesisroutesforthecompound9，andsuccessfullycompletetheroute3；andwedesignedtwosynthesisr

5、outesforcompound17，andsuccessfullycompletethesetworoutes．Inaddition，weexploredsomeimportantchemicalreaction，suchasbromination，Suzuki，Sonogashirareactions，ect．，intllefieldofmedicine，chemicalindustry,andfoundaoptimalmethodofpreparation．Meanwhile,withfluorineboronsaltassubstr

6、ateintheSuzukireaction，wefoundanovelcarbonchainextensionmethod．KEYwORDS：mGluR5Antagonist，SelaginellinL，ND-Selaginellin,MPEPaⅡ硕士学位论文目录目录摘!19l：⋯⋯⋯⋯．⋯⋯⋯⋯⋯⋯⋯⋯⋯．⋯⋯⋯⋯⋯⋯⋯．⋯．⋯⋯⋯⋯⋯⋯⋯⋯⋯．⋯．⋯⋯．⋯⋯．⋯⋯⋯⋯⋯．．．IABSTRACT⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯．⋯．⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯．⋯⋯⋯⋯⋯．⋯⋯．⋯⋯⋯⋯⋯⋯⋯．．．Ⅱ第一章概述⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯

7、⋯⋯⋯⋯⋯⋯⋯⋯．．11．1Selaginellin化合物结构及生物活性⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯．11．2SelaginellinL与mGluR5拮抗剂⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯．21．3mGluR5拮抗剂⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯．．31．3．1经典炔基型mGluR5拮抗剂⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯：⋯⋯⋯⋯⋯⋯．31．3．2新型非炔基mGluR5拮抗剂⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯5第二章目标化合物分子设计与合成路线⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯82．1分子设计⋯⋯⋯⋯⋯

8、⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯⋯．．82．1．1mGluR5拮抗剂的设计合成概况⋯⋯⋯⋯⋯⋯⋯⋯。⋯⋯j⋯“。⋯⋯．．．⋯⋯82．1．2Selaginellin类