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The[[SPI-QRYID1]] new insecticide oxazosulfyl has been discovered and developed by Sumitomo Chemical Co., Ltd., exhibiting excellent control against a broad range of important rice insect pests, including Hemiptera, Coleoptera, Lepidoptera, and Orthoptera. It has a novel structural backbone different from known insecticides and a new mode of action (MoA) classified by IRAC (Insecticide Resistance Action Committee) as the sole member of the novel main group 37, vesicular acetylcholine transporter (VAChT) inhibitors. Oxazosulfyl is also highly effective against the insect pests resistant to existing insecticides. In this chapter, discovery, chemical synthesis, and biological profile of oxazosulfyl are reported.