Study On The Technology Of Spiromesifen And Study On Synthesis And Biologocal Activity Of Novel Tetronic Acid Compounds

The insecticide acaricide spiromesifen,which belongs to tetronic acid derivatives discovered by Bayer CropScience,to promote in china in 2006,has an additional excellent activity against whiteflies and spider mites on cotton,vegetables and ornamental plants.The synthesis of spiromesifen reported in the literature is rare of domestic and many foreign patent documents is a simple description.Therefore,research and discussion on spiromesifen has better theoretical and economic significance.This article introduces two parts of the study on the technology of spiromesifen and study on synthesis and biologocal activity of novel tetronic acid compounds.The study on the technology of spiromesifen,adoping the cyclopentanone for the main beginning raw material,is given by the cyanic reation,hydrolysis,hydrolysis reation,the ester reation,condensation reation and acylnic reation.The process route from point of views of raw materials based on the domestic,low production costs,minimize environmental pollution and easy for industrial action.The reaction of each step discussion and comparison on details,to have the industrial feasibility,the key factors affect the reaction and process conditions to improve.The spiromesifen accords with export standard by this method,and it become competitive whether in appearance or in purity.Part of new commpound,in search for new acaricide with high activity,low toxicity,broad-spectrum and favorable safety profile,we designed 18 novel tetronic acid compounds in two series,using bioisosterism and union of active group on the base of the structure-activity relationship.This is summarized as follows:Their structures were confirmed by means of IR,1H NMR,MS and EA.The spatial configurations were studied by X-ray determination(two single crystals of these compounds were obtained).The relationship between structures and activities has been analyzed preliminarily.The results of acaricidal biological test show that most of these compounds possess good activity,and several have high potential value as novel acaricide.