N-甲基-4-氨基苯甲基磺酰胺的合成

合成药物舒玛普坦的重要中间体N-甲基-4-氨基苯甲基磺酰胺经以下四个步骤合成：对硝基氯化苄与亚硫酸氢钠反应生成对硝基苯甲磺酸，冰水浴中通氯气制得对硝基苯甲磺酰氯，氯仿为溶剂通甲胺气体进行甲胺氨化，水合肼还原得到N-甲基-4-氨基苯甲基磺酰胺，收率分别为90％，93％，60％，77％，产品结构经气一质谱、核磁谱图验证。该合成方法鲜见报道，且操作简单，所得产品纯度也较高，可以用来进一步合成药物舒马普坦。

Synthesis of N-Methyl-4-aminobenzyl Sulfonamide

N-Methyl-4-aminobenzyl sulfonamide, a key intermediate for synthesis of the pharmaceutical substance Sumatriptan, was prepared throught four steps. 4-Nitrobenzyl chloride was first converted to 4-nitrobenzyl sulphonic acid by reacting with sodium hydrosulfite, then the sulphonic acid obtained was oxidized to 4-nitrobenzyl sulfonyl chloride by chlorine, and N-methyl-4-nitrobenzyl sulfonamide was produced by reacting with methylamine, in the end, the title product was obtained by reducing the nitro group to amino group with hydrazine hydrate in the presence of iron trichoride on active carbon as the catalyst. The yields of the four steps are 90%, 93%, 60% and 77%, respectively. The intermediates and product were characterized by GC-MS and H~1NMR.