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Preliminary In Vivo Research On Pharmacodynamics Of Hirtellanine A And Platinum(?) Catalyzed Alkenes Isomerization

Posted on:2018-05-06Degree:MasterType:Thesis
Country:ChinaCandidate:J H MaFull Text:PDF
GTID:2404330596991088Subject:Medicinal chemistry
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The thesis contains two parts: Part 1.Preliminary in vivo research on pharmacodynamics of Hirtellanine A.Part 2.Platinum(IV)catalyzed alkenes isomerization.Part 1: Preliminary in vivo research on pharmacodynamics of Hirtellanine A.Hirtellanine A was isolated from the roots of Campylotropis hirtella by our research group.In vitro assay indicates that Hirtellanine A displays stronger B lymphocyte suppression activity and lower cytotoxicity,compared with cyclosporin A.However,the in vivo activity of this compound is unknown.Based on the previous synthetic studies,the reaction conditions and purification process were optimized and over 100 mg of Hirtellanine A was obtained.The preliminary evaluation of the efficacy of Hirtellanine A in mice was conducted.Part 2: Platinum(IV)catalyzed alkenes isomerization.Double-bond migration is an important method in organic synthesis.Usually,this reaction was promoted by the bases or transition metal complexes.However,each catalyst has their own drawbacks and may not suitable for all substracts.Herein,we present a novel platinum(IV)catalytic system for double-bond migration reaction.This catalytic system is efficient and has very high E/Z selectivity.The catalyst proved to be efficient for double bond migrate cross multiple carbon atoms.The newly formed double bond could conjugate not only with aromatic system,but also with carbonyl.More interestingly,the multiple double-bonds could also migrate into cyclohexane to form an aromatic compound,which provides a novel method for synthesizing aromatic compounds.
Keywords/Search Tags:Hirtellanine A, Synthetic route optimization, Efficacy evaluation, Platinum(?) as Catalysts, Isomerization of alkenes
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