Study On Synthetic Process Of Cycloxaprid

Cycloxaprid is a novel pesticide discovered by East China University of Science and Technology with independent intellectual property. With a unique structure, the novel neonicotinoid insecticide has shown excellent high insecticidal activities to the imidacloprid-resistant insects and it also has a good bioactivity against lepidoptera pests. It is being develop recently, process route optimization and producing-cost reduction are the key points of its commercialization and accessing to marketing.In this paper, the synthesis routes of cycloxaprid have been investigated and optimized the selected route in order to meet the requirement of industrillization. On the basis of the synthesis route in the literature, three viable process routes were designed according to the structure feature and some of the reactions in the route were optimized. The synthetic route was started from1,1-dichloroethylene. After nitrification, cyclization and condensation, CMNI was obtained. Then we got the target compound by the reaction of hydrolysis and cyclization reaction with2,5-dimethoxytetrahydrofuran and CMNI.The dissertation is mainly focused on the synthesis and work-up optimization of each step and different effects on the reactions were carried out. The production cost was reduced from1.69million RMB/t to0.87million RMB/t. The emission of methyl mercaptan and overuse of ethylene diamine were avoided. Because of its simplicity and mild conditions, the new process routes was prospective in industrial application and enviroment protection.