除草剂甲基二磺隆的合成

Synthesis of Mesosulfuron-methyl

摘要:

本文以对甲苯腈为原料，经氯磺化-氨解、氧化、还原、甲磺酰化、醇解反应制得关键中间体2-甲氧羰基-5-甲磺酰氨基甲基苯磺酰胺（6），6再与4,6-二甲氧基-2-(苯氧基羰基)氨基嘧啶反应得到目标产物甲基二磺隆（7），六步反应总收率33.3%，产物及中间体经IR，1H NMR，MS确证结构。与文献合成工艺比较，该方法具有原料易得，操作简便，收率高等优点，工业化应用前景高。

Abstract:

In this paper, the key intermediate of 2-methoxylcarbonyl-5-methylsulfonylaminomethylbenzene sulfonamide (6) was prepared starting from p-tolunitrile via chlorosulfonation-aminiation, oxidation, reduction, methlsulfonylation and alcoholysis. Subsequently, the aimed product of mesosulfuron-methyl (7) was achieved from 6 and 4,6-dimethoxy-2-(phenoxycarbonyl)aminopyrimidine, the total yield of the six-steps was 33.3%. The structures of target product and intermediates were determined by IR, 1H NMR and MS. Compared with the synthesis process in references, this synthetic route is cost-effective, simple operation, high yield and valuable for the industrial application.