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Total Synthesis Of(-)-N-acetylcolchinol And Modification Ofα-Mangostin’s Structure

Posted on:2013-09-13Degree:MasterType:Thesis
Country:ChinaCandidate:Q P HuFull Text:PDF
GTID:2234330371969133Subject:Pharmacy
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This thesis contains two parts:(1) Asymmetric Synthesis of (-)-N-acetylcolchinol, a derivative of Colchicine; (2) a-Mangostin was separated from the Mangosteen Garcinia angostana as the main component and a series of derivatives were synthesized.Part I:The Colchicine derivatives have the excellent anti-tumor biological activity. Among them, (-)-N-acetylcolchinol was a kind of new targeting agent with the unique anti-angiogenic activity. In this part, the asymmetric synthesis of (-)-N-acetylcolchinol was explored. Highly enantioselective alkynylation of aldehydes catalyzed by a readily available chiral amino alcohol-based ligand was applied to construct the chiral center. And the construction of the seven-member ring was attempted to be constructed by C-H activation catalyzed by mental.Part II:a-Mangostin is the main component extracted from the shell of Mangosteen Garcinia angostana. Great attention has been paid on its physiological activity, since it has a structure of benzchromone with phenolic hydroxy groups. The thesis discusses the project on the new synthesis of seven a-Mangostin analogues based on the structure of benzchromone of a-Mangostin, among which derivatives that have strong physiological activity may be discovered. Further research on the activity of this kind of derivatives is under way.
Keywords/Search Tags:alkynylation of aldehydes, (-)-N-acetylcolchinol, α-Mangostin
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