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[目的]甲磺胺磺隆是一种高效、广谱、低毒、高选择性的磺酰脲类除草剂。综述甲磺胺磺隆重要中间体2-氨磺酰基-4-甲磺酰氨基甲基苯甲酸甲酯的合成方法,并对其中一种合成路线进行详细的研究。[方法]以对甲苯腈为起始原料,经过硝化、氧化、酯化、加氢、磺酰化、重氮化和氨化7步反应得到产物。[结果]在优化的反应条件下,以对甲苯腈计总收率可达31.3%。[结论]该工艺路线具有反应条件温和、产品纯度高、易于实现工业化生产等特点。
[Objective] Mesythonin is an efficient, broad spectrum, low toxicity and high selectivity sulfonylurea herbicide. In this paper, the synthesis method of methyl 2-sulfamoyl-4-methanesulfonamidomethylbenzoate, an important intermediate of sulfamethoxazole, was reviewed. And one of the synthetic routes was studied in detail. [Method] With p - Toluene nitrile as starting material, the product was obtained by nitration, oxidation, esterification, hydrogenation, sulfonylation, diazotization and ammonification. [Result] Under the optimal reaction conditions, the total yield of p-tolunitrile was 31.3%. [Conclusion] The process route has the characteristics of mild reaction conditions, high product purity and easy realization of industrialized production.