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首页> 外文期刊>Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry >Synthesis, Biological Activity of Pyrimidine Linked with Morpholinophenyl Derivatives
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Synthesis, Biological Activity of Pyrimidine Linked with Morpholinophenyl Derivatives

机译:嘧啶与吗啉代苯基衍生物连接的合成及生物活性

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摘要

A new series of 5-fluoro-N-4-(3-(4-substitutedbenzylamino)phenyl)-N-2-(4-morpholinophenyl)pyrimidine-2,4-diamine derivatives (7a-j) are prepared from using an intermediate compound 5-fluoro-N-4-(3-(aminophenyl)-N-2-(4-morpholinophenyl) pyrimidine-2,4-diamine (5). The structures of the newly synthesized products are established from their spectral H-1-NMR, C-13-NMR, F-19-NMR, ESI-MS, and analytical data. Here we report the synthesized compounds and larvicidal activity. All the compounds are screened for their significant larvicidal activity against third instar larvae at 24, 48, and 78-h time exposure, and values were compared with standard drug Malathion. The Compounds 7i, 7a, 7c, 7f, and 7j exhibited significant activity. However the compounds 7b, 7e, 7d, and 7h showed excellent activity when compared to the above compounds and to standard drug malathion too because of the presence of mild electron withdrawing groups such as trifluoro, fluorine, hydroxy, nitro, and methoxy derivatives which are attached to the benzyl ring.
机译:新型的5-氟-N-4-(3-(4-取代的苄基氨基)苯基)-N-2-(4-吗啉代苯基)嘧啶-2,4-二胺衍生物(7a-j)的制备是通过使用中间体化合物5-氟-N-4-(3-(氨基苯基)-N-2-(4-吗啉代苯基)嘧啶-2,4-二胺(5)。新合成产物的结构由其光谱H确定-1-NMR,C-13-NMR,F-19-NMR,ESI-MS和分析数据。这里我们报告合成的化合物和杀幼虫活性。筛选了所有化合物对三龄幼虫的显着杀幼虫活性分别与24小时,48小时和78小时的暴露时间进行比较,并将其值与标准药物马拉硫磷进行比较,化合物7i,7a,7c,7f和7j表现出明显的活性,而化合物7b,7e,7d和7h表现出优异的活性。与上述化合物和标准药物马拉硫磷相比,由于存在温和的吸电子基团(例如三氟,氟,羟基,硝基和甲氧基衍生物),连在苄环上的

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