[Aims]This study aims to afford a new approach for the synthesize of dimesulfazet,a sulfonamide herbicide for paddy.[Methods]A new synthetic route for dimesulfazet was designed,using 2-(aminomethyl)aniline as the starting material.The target product was obtained through 5 steps,including BOC-protection of benzylamine,sulfonylation of aniline,BOC-deprotection,amidation and intramolecular cyclization.[Results]The total yield of the new synthesized method was 48％and the structure of the target product was characterized by HRMS,1H NMR and 13C NMR.We investigated the optimum reaction condition for the sulfonation of aniline to obtain the optimal reaction systems:using trifluoromethanesulfonic anhydride as the sulfonation reagent,triethylamine as the binding agent,and dichloromethane as the solvent.A suitable amount of anhydride and base could improve the reaction conversion rate and reduce the generation of by-products,thereby increasing the yield.[Conclusions]The synthetic route has the advantages of short steps,available raw materials,simple operation methods and mild conditions.The whole process is suitable for laboratory operation.
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