Design,synthesis and insecticidal activity of benzothiazole derivatives
[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.