除草剂甲基二磺隆的合成

该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(Ⅵ),Ⅵ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(Ⅶ),6步反应总收率33.3%,产物及中间体经IR、1HNMR、MS确证结构。与文献合成工艺比较,该法具有原料易得,操作简便,收率高等优点。

Synthesis of Mesosulfuron-methyl

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.