农药2024,Vol.63Issue(1) :8-12.DOI:10.16820/j.nyzz.2024.0103

苯并噻唑类化合物的设计合成及杀虫活性

Design,synthesis and insecticidal activity of benzothiazole derivatives

韩金龙 徐靖博 常秀辉 解喜山 吴鸿飞
农药2024,Vol.63Issue(1) :8-12.DOI:10.16820/j.nyzz.2024.0103

苯并噻唑类化合物的设计合成及杀虫活性

Design,synthesis and insecticidal activity of benzothiazole derivatives

韩金龙 1徐靖博 1常秀辉 1解喜山 1吴鸿飞1
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作者信息

  • 1. 沈阳中化农药化工研发有限公司新农药创制与开发国家重点实验室,农药国家工程研究中心,沈阳 110021
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摘要

[目的]发现结构新颖的高杀虫活性化合物.[方法]将苯并噻唑活性亚结构引入间位双酰胺骨架结构中,以2-溴苯胺或2-二氟甲氧基苯胺为原料,经七氟异丙基化、溴化、酰胺化等8步反应,合成一系列新型苯并噻唑类化合物,并对其进行杀虫活性测试.[结果]室内生测结果表明:目标化合物对黏虫和小菜蛾具有优异的杀虫活性,尤其是化合物k1、k3和k9在5 mg/L质量浓度下对黏虫和小菜蛾的致死率均为90%以上.[结论]化合物k1、k3和k9可以作为候选化合物深入研究,或为发现高活性化合物作为先导化合物进一步结构优化研究.

Abstract

[Aims]The aim was to discover novel compounds with excellent insecticidal activities.[Methods]A series of benzothiazole derivatives were synthesized by the introduction of benzothiazole active substructures into metadiamide scaffolds.The compounds were prepared from 2-bromoaniline or 2-difluoromethoxyaniline through 8-step reactions including heptafluoroisopropylation,bromination and amidation,and their insecticidal aitivities were tested.[Results]The bioassay results in greenhouse showed that these target compounds exhibited excellent insecticidal activities against Mythimna separate and Plutella xylostella,especially compounds k1,k3 and k9 with mortality rates over 90%against the two pest insects at 5 mg/L.[Conclusions]Compounds k1,k3 and k9 could be candidates for further study or lead compounds for further structural optimization for discovery of compounds with high bioactivities.

关键词

苯并噻唑/合成/杀虫活性

Key words

benzothiazole/synthesis/insecticidal activity

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出版年

2024
农药
沈阳化工研究院有限公司

农药

CSTPCDCSCD北大核心
影响因子:0.665
ISSN:1006-0413
参考文献量13
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