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Position: Home > Articles > Synthesis and Antifungal Activity Study of a Series of Novel Pyridine Linked Fluorinated Pyrazole Derivatives Agrochemicals 2012,51 (9) 22-24+30

含氟吡啶联吡唑类衍生物的合成及生物活性

作  者:
蔡飞;郑志文;姬文娟;邢家华;孔小林
单  位:
浙江省化工研究院;浙江工业大学化学工程与材料学院中化蓝天浙江省化工研究院有限公司;浙江省化工研究院有限公司
关键词:
吡啶;吡唑;合成;杀菌活性
摘  要:
[目的]发现具有生物活性新化合物。[方法]以2,6-二氯吡啶(1)为起始原料,经肼基化、环合、水解和酰氯化反应,生成中间体1-(6-氯-2-吡啶)-5-二氟甲基-1H-吡唑-4-甲酰氯(6),化合物6与取代苯胺(7)反应,制得14个含氟吡啶联吡唑类未见报道的目标化合物。[结果]通过1H NMR和LC-MS表征,初步生物活性测定结果表明在500 mg/L质量浓度下,目标化合物对黄瓜霜霉病菌、黄瓜白粉病菌、黄瓜灰霉病菌均有一定抑制作用,部分化合物对黄瓜霜霉病菌、黄瓜白粉病菌、黄瓜灰霉病菌抑制率达85.0%以上。[结论]此类含氟吡啶联吡唑类化合物有较好的抑制真菌活性。
译  名:
Synthesis and Antifungal Activity Study of a Series of Novel Pyridine Linked Fluorinated Pyrazole Derivatives
作  者:
CAI Fei1,ZHENG Zhi-wen2,JI Wen-juan2,XING Jia-hua2,KONG Xiao-lin1,2,TAN Cheng-xia1,XU Tian-ming2(1.college of chemical engineering and materials science,Zhejiang University of Technology,hangzhou 310014,china;2.Zhejiang Base of National southern Pesticide research centre,sinochem lantian Zhejiang research institute of chemical industry co.,ltd.,hangzhou 310023,china)
关键词:
pyridine;pyrazole;synthesis;antifungal activity
摘  要:
[Aims] The aim is to discover new compounds with biological activity.[Methods] 1-(6-chloropyridin-2-yl)5-difluoromethyl-1h-pyrazole-4-carbonyl chloride(6) was synthesized using 2,6-dichloropyridin as raw materials by hydraztion,cyclization,hydrolysis and acyl chlorination.Then 14 novel title compounds were synthesized by acylation of(6) with substituted anilines(7).[Results] The structures of the title compounds were confirmed by lc-ms and 1h Nmr,antifungal activity test showed that 14 compounds exhibited some inhibiting effect against all the tested strains at the concentration of 500 mg/l,and some compounds showed good fungicidal activity against B.lactuca,s.fuliginea,and B.cinerea with more than 85% control.[Conclusions] These pyridine linked fluorinated pyrazole derivatives have good antifungal activities.

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