Study On The Synthetic Process Of Cyflumetofen

Cyflumetofen,one of the benzoyl cyanide acaricides,was developed by Japan,and registered for sale in 2007.It can be used to control phytophagous mites in fruit trees,tea trees,ornamental plants,etc.And it has a great potential in the market of acaricide.In this paper,according to the existing literature on the synthesis of Cyflumetofen and its intermediates at home and abroad,a new process route for the synthesis of Cyflumetofen was designed by analyzing and summarizing its strong points to offset its weakness.On this basis,the "synthetic process optimization method and principle" is used to explore and study the reaction conditions of each step from the local and global point of view,so that it can be suitable for industrial production of different scale.O-trifluoromethylbenzoic acid is the main intermediate for the synthesis of Cyflumetofe and related drugs,but there is no large-scale production in China.In this paper the synthesis process of O-trifluoromethylbenzoic acid was studied:O-trifluoromethylbenzoic acid was synthesized from 2-chloro trifluoromethyl benzene by Grignard reaction,addition reaction and hydrolysis reaction.The total yield of O-trifluoromethyl benzoic acid was 41.3% based on 2-chloro trifluoromethyl benzene,and the purity was 99.5%.In this thesis,the synthesis process of Cyflumetofen was studied: using4-tert-Butylphenyl acetonitrile as the raw material,.and the target product was obtained by condensation reaction,transesterification reaction,and acylation reaction.The total reaction yield was 63.1% based on 4-tert-Butylphenyl acetonitrile,and the purity was99.2%.The research and optimization of the synthesis process involves the selection and determination of the process conditions in each step of the reaction.And its core basis is under the premise of increasing the content of the main product,how to select and design the ideal process conditions to minimize control the occurrence of major side reactions in each step.So as to that improve the selectivity of the main reactions.Based on the principle of process optimization,this paper discusses and analyzes the process conditions involved in each step of the reaction.The conditions include analysis of side reactions,screening of reaction materials,determination of material ratio,selection of solvents,selection of temperature,selection of feeding order,selection and determination ofpost-processing methods,etc.The synthesis process proposed in this paper has the characteristics of high yield,simple operation,high purity of the obtained product,and suitable for industrial production.