The first neonicotinoid insecticide, Imidacloprid, which was developed by Bayer AG in middle 1980s, has been one of the most successful novel insecticides. Represented by Imidacloprid, the neonicotinoid insecticides were featured with high insecticidal activities, broad insecticidal spectra, low mammalian and aquatic toxicity, favorable systemic properties, proper field stability, and environmental friendliness. Therefore, the neonicotinoid insecticides have become one of the most important hot areas in insecticidal innovation. Afterwards, a series of neonicotinoid insecticides, such as Thiacloprid, Clothianidin, Thiamethoxam, Acetamiprid, Nitenpyram and Dinotefuran, were developed (EP 247477, 296453, 685477, 235725, 235725, 315826, 192060, 244777, 0386565, 580553, and 1031566, JP 62292765, 8259568, 8291171, and 7242633).
However, the application of these compounds was somehow limited due to the serious resistance caused by frequent use of and cross-resistance between these neonicotinoid insecticides having high structural similarity, which were also the important reasons that restrict further development of neonicotinoid insecticides. Meanwhile, the selectivity for insect control was limited by a narrow insecticide controlling spectrum as the neonicotinoid insecticides were mainly high active on Homoptera and Lepidoptera pests.
Thus, the main technical problem to be solved by the present invention is to develop novel and more effective insecticides by the structural modification of nitromethylene compounds so as to resolve the resistance issue, broaden the insecticidal spectrum and make the novel compounds applicable as insecticides.
USPTO Backgrounds
USPTO Backgrounds