对甲苯磺酰甲基异腈的合成

Synthesis of p-Tolylsulfonylmethyl Isocyanide

[目的]合成制备许多新型杂环农药的一个重要中间体对甲苯磺酰甲基异腈。[方法]以对甲苯亚磺酸钠为原料,经类似Mannich缩合和酰胺脱水反应制得对甲苯磺酰甲基异腈。[结果]在优化的条件下,反应总收率为72.3%(以对甲苯亚磺酸钠计),含量为98.5%,其结构经1H NMR分析确证。[结论]该工艺收率高、操作简单、条件温和,可为工业化生产提供参考。

[Aims] The aim is to prepare p-tolylsulfonylmethyl isocyanide, a key intermediate for synthesizing many new heterocyclic pesticides. [Mothods] p-Tolylsulfonylmetjhyl isocyanide was obtained trough resembling Mannich and hydrolysis reactions using sodium p-toluenesulfinate as starting material. [Results] The total yield was 72.3% based on sodiump-toluenesulfinate under the optimized reaction conditions and purity was 98.5%. The structure of the product was confirmed by 1H NMR. [Conclusions] The synthetic process has advantages of high yield, simple operation and safety, which is an important directive to industrialized production.