唑尼沙胺的新合成方法  

Novel Synthesis Method of Zonisamide

作　　者：曾宪烜 刘伟锋 刘地发 Zeng Xianxuan;Liu Weifeng;Liu Difa(Jiangxi Qingfeng Phannaceutical Co.,Ltd.,Ganzhou 341000,China)

机构地区：[1]江西青峰药业有限公司,江西赣州341000

出　　处：《山东化工》2024年第1期73-77,87,共6页Shandong Chemical Industry

摘　　要：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。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.

关 键 词：唑尼沙胺 叔丁胺 脱保护 癫痫 合成 

分 类 号：TQ226.3[化学工程—有机化工] O625.5[理学—有机化学]