Synthesis, Structure and Biological Activities of Novel 2-(Trifluoromethyl)-6-arylimidazo2,1-b1,3,4-thiadiazole (bis-)Mannich Base Derivatives Containing Substitutedpiperazine Moiety

摘要

A convenient and practicable method for the synthesis of the novel 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4]-thiadiazole (bis-)Mannich base derivatives containing various substitutedpiperazine motif has been developed based on the fused-heterocycle intermediate.The new structures were identified through melting points,1H NMR,13C NMR,19F NMR,elemental analysis (or HRMS) and X-ray single-crystal diffraction.The pesticidal bioassays showed that some of compounds exhibited good fungicidal activities against Cercospora arachidicola,Physalospora piricola and Rhizoctonia cereali at 50 mg/L;some of them displayed favourable insecticidal activities against oriental armyworm (Mythimna separata Walker) at 200 mg/L,particularly,Vk and Vm with mortality rate of 75％ and 80％ respectively,could be considered as new insecticidal lead compounds for further structural optimization.