N-(2-(腈基(4,6-二甲氧基嘧啶-2-基)甲基)苯基)酰胺类衍生物的合成及生物活性

doi:10.3724/SP.J.1095.2013.20541

摘要/Abstract

摘要： 以2-(2-硝基苯基)乙腈及4,6-二甲氧基-2-甲磺酰基嘧啶为起始原料，分别经缩合、还原及酰胺化反应合成了6个未见文献报道的N-(2-(腈基(4,6-二甲氧基嘧啶-2-基)甲基)苯基)酰胺类衍生物，其结构经1H NMR、MS和元素分析进行了确证。在150 g/hm2的用量条件下，合成化合物未显示出除草活性。在200 mg/L浓度下，部分化合物对黄瓜灰霉病及水稻纹枯病表现出一定的抑菌作用，其中化合物4d对水稻纹枯病的抑制率为72.33%。

关键词: 嘧啶水杨酸, 二甲氧基嘧啶, 酰胺, 合成, 生物活性

Abstract: Six novel N-(2-(cyano(4,6-dimethoxypyrimidin-2-yl)methyl)phenyl) substitued amide derivatives were synthesized using 2-(2-nitrophenyl)acetonitrile and 4,6-dimethoxy-2-(methylsulfonyl)pyrimidine as starting materials by condensation reaction, reduction reaction and acylation reaction, respectively. The structures of all synthesized compounds were determined by 1H NMR, MS and elemental analysis techniques. As-synthesized compounds did not show herbicidal activities at 150 g/hm2. The antibacterial activity test indicated that some of them exhibited certain inhibitory activities against Sphaerotheca fuliginea and Rhizoctonia solani, respectively at 200 mg/L. The inhibition rate of compound 4d against Rhizoctonia solani was 72.3% at 200 mg/L.

Key words: pyrimidinylsalicylic acid, dimethoxypyrimidine, Acidamide, synthesis, Bioactivity

中图分类号:

O621.2

李元祥, 陈迪钊. N-(2-(腈基(4,6-二甲氧基嘧啶-2-基)甲基)苯基)酰胺类衍生物的合成及生物活性[J]. 应用化学, DOI: 10.3724/SP.J.1095.2013.20541.

LI Yuanxiang1,2*, CHEN Dizhao1. Synthesis and Biological Activities of N-(2-(Cyano(4,6-dimethoxypyrimidin-2-yl)methyl)phenyl) Substitued Amide Derivatives[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2013.20541.

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