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杂环合成中的烯胺腈:含苯并噻唑部分的一些新吡唑、异噁唑和嘧啶衍生物的合成及抗菌评价。

Enaminonitrile in heterocyclic synthesis: synthesis and antimicrobial evaluation of some new pyrazole, isoxazole and pyrimidine derivatives incorporating a benzothiazole moiety.

机构信息

Department of Chemistry, Faculty of Science, Mansoura University, ET-35516 Mansoura, Egypt.

出版信息

Eur J Med Chem. 2009 Dec;44(12):4813-8. doi: 10.1016/j.ejmech.2009.07.024. Epub 2009 Jul 30.

Abstract

Enaminonitrile 2 was used as key intermediate for the synthesis of polyfunctionally substituted heterocycles (e.g. pyrazoles, isoxazole, pyrimidines, thiazolo[3,2-a]pyrimidine, tetrazolo[1,5-a]pyrimidine, pyrido[1,2-a]pyrimidine, 1,5-benzodiazepine, and pyrazolo[1,5-a]pyrimidine) incorporating benzothiazole moiety via its reactions with some N-nucleophiles. The newly synthesized compounds were characterized by IR, (1)H NMR and mass spectral studies. Representative compounds of the synthesized products were tested and evaluated as antimicrobial agents.

摘要

烯胺腈 2 被用作合成多官能取代杂环(如吡唑、异噁唑、嘧啶、噻唑并[3,2-a]嘧啶、四唑并[1,5-a]嘧啶、吡啶并[1,2-a]嘧啶、1,5-苯并二氮杂䓬和吡唑并[1,5-a]嘧啶)的关键中间体,这些杂环通过与一些 N-亲核试剂的反应引入苯并噻唑部分。新合成的化合物通过红外光谱、(1)H NMR 和质谱研究进行了表征。对合成产物的代表性化合物进行了测试和评估,作为抗菌剂。

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