含苯基吡啶基团的肟醚乙酸酯类化合物的合成与抑菌活性  

Synthesis and fungicidal activity of novel methoximinoacetates containing phenylpyridine moieties

作　　者：毛达杰[1,2] 胡崇波[1] 刘建华[1] 杜晓华[1] 徐振元[1] 

机构地区：[1]浙江工业大学催化加氢研究中心、浙江省绿色农药清洁生产技术研究重点实验室,杭州310014 [2]中化宁波(集团)有限公司,浙江宁波315000

出　　处：《农药学学报》2014年第4期406-413,共8页Chinese Journal of Pesticide Science

摘　　要：以3-羟基苯硼酸和取代含溴吡啶为原料,经Suzuki偶联和亲核取代两步反应合成了24个未见报道的含苯基吡啶基团的肟醚乙酸酯类化合物,其结构均通过1H NMR、ESI-MS和IR确证。初步生物活性测定结果表明,大部分目标化合物具有一定的抑菌活性,其中化合物5i、5r、5t在50 mg/L下对黄瓜霜霉病菌的抑制率达到80%。说明此类化合物具有作为杀菌剂先导进行进一步结构优化的潜力。Twenty four novel methoximinoacetate compounds containing phenylpyridine moieties were synthesized from （ 3-hydroxyphenyl ） boric acid and substituted bromopyridines via Suzuki cross-coupling reaction and nucleophilic substitution. The structures of all compounds were confirmed by 1 H NMR, ESI-MS and IR. Bioactivity tests showed that most of the compounds have moderate to good fungicidal activity and compounds 5i, 5r and 5t exhibited more than 80% inhibition against Pseudoperonospora cubensis at 50 mg/L, which means that the title compounds are potential as the fungicidal lead compounds.

关 键 词：苯基吡啶 肟醚乙酸酯 合成 抑菌活性 黄瓜霜霉病菌 

分 类 号：O626.32[理学—有机化学] S482.2[理学—化学]