Design,synthesis and insecticidal activities of novel anthranilic diamides containing polyfluoroalkyl pyrazole moiety

In order to discover new molecules with good insecticidal activities, a series of anthranilic diamides containing polyfluoroalkyl pyrazole were designed and synthesized, and their structures were characterized by1 H NMR and HRMS. Bioassays demonstrated that some of the title compound exhibited excellent insecticidal activities. The larvicidal activities of compound 8a, 8c, 8g, 8k and 8l against Mythimna separata Walker were 100% at 0.8 mg/L. The insecticidal activities of compound 8a, 8c,8e, 8g, 8k and 8l against Plutella xylostella Linnaeus were 100% at 0.4 mg/L. Surprisingly compounds 8a and 8c still showed 100% larvicidal activities against Plutella xylostella Linnaeus at 0.08 mg/L comparable to the commercialized Chlorantraniliprole. The LC_（50） of compound 8a and 8c against M. separata is 0.048 and 0.043 mg/L respectively.

The exploration of chiral N-cyano sulfiliminyl dicarboxamides on insecticidal activities

Due to new mechanism of action and ecofriendly characteristics,dicarboxamide insecticides have attracted more and more attentions in modern pest management.A series of 20 dual chiral N-cyano sulfilimines containing two centers（carbon and sulfur） were designed and synthesized.All title compounds were determined by ^1H NMR,high-resolution mass spectrometry（HRMS） and optical polarimeter.The preliminary results indicated that some of them exhibited favourable insecticidal activities against oriental armyworm（Pseudaletia separata Walker）.These isomers exhibited different impact on activity following the sequence as（Sc,Ss） 〉（Sc,Rs）,and the rule of title compounds＇ activity against oriental armyworm was 3-CF3≥2—CH3—4—Cl〉2,3,4-trifluro in the anilide moiety.The results indicated that these groups such as 3-CF3,2—CH3—4—Cl or 2,3,4-trifluro were inefficient to replace heptafluoroisopropyl group for high larvicidal activity,which provided some guidance for the further modifications of sulfiliminyl dicarboxamides.

Design,Synthesis,Biological Evaluation and SARs of Anthranilic Diamide Derivatives Containing Pyrrole Moieties

In order to find a new variety of ryanodine receptor(RyR)regulator with greater biological activity,a se-ries of anthranilic diamide derivatives possessing pyrrole structure was designed and synthesized in this study.The pyrrole derivatives were evaluated for their insecticidal activity against Mythimna separata and Plutella xylostella.As indicated by the preliminary biological activities,compounds 12h-12j and 121-12n exhibited a remarkable in-secticidal activity against M.separata at 0.25 mg/L.Compared to control chlorantraniliprole.compound 12i exhibited more excellent insecticidal activity at 0.1 mg/L.Meanwhile,compounds 12c,12h,12i.12j.121,and 12m were selected to test the insecticidal activity against P xylostella,which led to the desirable insecticidal activity at 1x103 mg/L.Notably,compound 121 demonstrated 47%insecticidal activity at 5×10^(-6) mg/L over the control.In addition,the biological mechanism of action of compound 12i was investigated by means of insect clectrophysiology experiment.