农药学学报
農藥學學報
농약학학보
CHINESE JOURNAL OF PESTICIDE SCIENCE
2014年
4期
406-413
,共8页
毛达杰%胡崇波%刘建华%杜晓华%徐振元
毛達傑%鬍崇波%劉建華%杜曉華%徐振元
모체걸%호숭파%류건화%두효화%서진원
苯基吡啶%肟醚乙酸酯%合成%抑菌活性%黄瓜霜霉病菌
苯基吡啶%肟醚乙痠酯%閤成%抑菌活性%黃瓜霜黴病菌
분기필정%우미을산지%합성%억균활성%황과상매병균
phenylpyridine%methoximinoacetate%synthesis%fungicidal activity%Pseudoperonospora cubensis
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1 H 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。
以3-羥基苯硼痠和取代含溴吡啶為原料,經Suzuki偶聯和親覈取代兩步反應閤成瞭24箇未見報道的含苯基吡啶基糰的肟醚乙痠酯類化閤物,其結構均通過1 H NMR、ESI-MS和IR確證。初步生物活性測定結果錶明,大部分目標化閤物具有一定的抑菌活性,其中化閤物5i、5r、5t在50 mg/L下對黃瓜霜黴病菌的抑製率達到80%。說明此類化閤物具有作為殺菌劑先導進行進一步結構優化的潛力。
이3-간기분붕산화취대함추필정위원료,경Suzuki우련화친핵취대량보반응합성료24개미견보도적함분기필정기단적우미을산지류화합물,기결구균통과1 H NMR、ESI-MS화IR학증。초보생물활성측정결과표명,대부분목표화합물구유일정적억균활성,기중화합물5i、5r、5t재50 mg/L하대황과상매병균적억제솔체도80%。설명차류화합물구유작위살균제선도진행진일보결구우화적잠력。
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.