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...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 rag/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.展开更多
基金This work was supported by the National Key Research and Development Program of China （No. 2017YFD0200505）, the National Natural Science Foundation of China （Nos. 21372133 and 21772103）, and Tianjin Natural Science Foundation （No. 17JCYBJC19900）. We thank the teachers of the Biological Assay Center, Nankai University, for kind bioassay assistance of compounds.
文摘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 rag/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.
