144172-26-9Relevant articles and documents
Synthesis process of indoxacarb
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, (2020/05/30)
The invention discloses a synthesis process of indoxacarb. The method comprises the following steps: reacting m-chlorobenzaldehyde serving as a raw material with malonic acid to remove monomolecular water and carbon dioxide to generate an intermediate SRCA, performing a hydrogenation reduction on the intermediate SRCA in an autoclave in the presence of a catalyst to obtain an intermediate SRCH, and cyclizing the SRCH by using hydrogen fluoride as a dehydrating agent to obtain the final product indoxacarb. The synthesis process is simple and easy to implement, energy is saved, consumption is reduced, the yield is increased, and good economic and environmental benefits are obtained.
Oxadiazine cinnamate derivatives as well as preparation method and application thereof
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, (2018/07/30)
The invention provides oxadiazine cinnamate derivatives as well as a preparation method and application thereof. The molecular structures of the oxadiazine cinnamate derivatives are shown in a formula(I) described in the description, wherein R1 is hydrogen, halogen, an alkyl group having 1-4 carbon atoms, alkoxy having 1-4 carbon atoms or an amino group; R2 is -CF3, -OCF3 or -OCH2F. The preparation method provided by the invention combines indoxacarb with cinnamic acid so as to obtain the oxadiazine cinnamate derivatives by rationally designing the structure of the indoxacarb; the oxadiazinecinnamate derivatives not only can significantly increase the poisonous activity of prodenia litura, but also has good biological activity against mosquitoes with drug resistance; compared with commercial indoxacarb insecticide, the poisonous activity of the compounds against pests is greatly enhanced, and the biological activity of the compounds for drug-resistant pests is especially enhanced, sothat drug protection is provided for the prevention and control of the resistant pests. Furthermore, the raw materials used in the method for producing the compounds provided by invention are readilyavailable, the reaction conditions are mild, and the yield of the target product is high.
Design, synthesis and structure-activity relationship of indoxacarb analogs as voltage-gated sodium channel blocker
Hao, Wenbo,Fu, Chunling,Yu, Huijuan,Chen, Jian,Xu, Hanhong,Shao, Guang,Jiang, Dingxin
supporting information, p. 4576 - 4579 (2015/10/12)
Indoxacarb, the first commercialized pyrazoline-type sodium-channel blocker, is a commonly used insecticide because of high selectivity. To discover sodium-channel blocker with high insecticidal activity, a series of novel indoxacarb analogs were designed and synthesized by judicious structural modifications of the substituent group of C5, C6 in indenone and C′4 in benzene ring. Some analogs exhibited significant insecticidal activities against Spodoptera litura F. and excellent BgNav1-1a channel inhibitory activity. The structure-activity analysis indicated that the presence of strong electron-withdrawing group and decreased steric hindrance of indenone ring (R1, R2) in 5- and 6-position could enhance larvicidal activity and BgNav1-1a channel inhibitory activity.
