以1,2-苯并异噁唑-3-甲磺酸钠盐为起始物料,经过氯化亚砜酰氯化,叔丁胺酰胺化保护,并在盐酸条件下脱去叔丁基,粗品经过甲醇精制,最终得到目标化合物唑尼沙胺(Zonisamide).产物经1 H NMR、13 C NMR、MS及XRD进行结构确证,该合成工艺条件温和、操作简便、三废量少,且产品质量好,适合工业化生产.
Abstract
Using 1,2-Benzisoxazole-3-methanesulfonic acid sodium salt as the starting material,Zonisamide was synthesized by chlorination with thionyl chloride,followed by sulfonamidation with tert butylamine,and directly tert-butyl deprotection to afford crude product,then refined from methanol.The product structure was confirmed by 1 H NMR,13 C NMR,MS and XRD.The synthesis method was demonstrated to be a good process to afford high quality API with its remarked features,such as mild condition,easily operated and less industrial wastes.
维普
万方数据