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首页> 外文期刊>Pharmaceutical Chemistry Journal >Synthesis and Antibacterial Activity of 2-[2,2-Dimethyl-4(3-Trifluoromethylphenyl)-Tetrahydropyran-4-Yl]Arylamine Oxalates
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Synthesis and Antibacterial Activity of 2-[2,2-Dimethyl-4(3-Trifluoromethylphenyl)-Tetrahydropyran-4-Yl]Arylamine Oxalates

机译:2- [2,2-二甲基-4(3-三氟甲基苯基)-四氢吡喃-4-Yl]芳胺草酸酯的合成及抑菌活性

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摘要

Interaction of ethylcyano(2,2-dimethyltetrahydro-2H-puran-4-yl)acetate with 3-trifluoromethylphenylmagnesium bromide yielded cyanoesters, decarbethoxylation of which produced the corresponding nitrile. Reduction of the latter with LiAlH4 led to the formation of 2-[2,2-dimethyl-4-(3-trimethylphenyl)tetrahydropyran-4-yl]ethylamine. Interaction of the resulting amine with aromatic aldehydes produced azomethines, which were reduced with NaBH4 to secondary amines, which were then converted to the oxalates. Several of these were found to have high levels of antibacterial activity.
机译:氰基乙基(2,2-二甲基四氢-2H-呋喃-4-基)乙酸乙酯与3-三氟甲基苯基溴化镁的相互作用产生氰基酯,其脱碳乙氧基化反应生成相应的腈。用LiAlH 4还原后者导致2- [2,2-二甲基-4-(3-三甲基苯基)四氢吡喃-4-基]乙胺的形成。所得胺与芳族醛的相互作用产生了甲亚胺,将其用NaBH4还原为仲胺,然后将其转化为草酸酯。发现其中一些具有高水平的抗菌活性。

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