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Synthesis And Structural Confirmation Of 2-Alkoxy/aroxy-1,2,4-triazolo [1,5-a] Pyrimidines

Posted on:2004-06-13Degree:MasterType:Thesis
Country:ChinaCandidate:H WangFull Text:PDF
GTID:2121360092993269Subject:Organic Chemistry
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The research progress of four kinds of famous ALS inhibitors containing sulfoylureas, l,2,4-tria2olo[l,5-a]pyrirnidine-2-sulforiamides, imidazolinones and pyrimidinyl (thio)ethers was reviewed in this thesis.Based on the studies of structure-activity relationship and the analysis of electrostatic potential, the method of bioisoteric substitution was applied for designing and synthesizing two series of new compounds to explore novel derivatives of pyrimidinylethers containing heterocycles which have higher biological activity. The structures of the target compounds have been confirmed by 1H NMR and MS, which can be devided into two series according to their structures categories, shown as follows:1.2-alkoxy/aroxy-5 7-dimethyl-1,2,4-triazolo[1l,5-a]pyriniiduies (I)2.2-alkoxy/aroxy-5,7-dimethoxy-1,2,4-triazolo[1,5-a]pyrirnidines (II)...
Keywords/Search Tags:ALS inhibitors, 1,2,4-triazolo[1,5-a]pyrimidines, bioisoterism substitution, rational design, structure-activity relationship, synthesis
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