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唑尼沙胺的新合成方法

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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。
Novel Synthesis Method of Zonisamide
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.

Zonisamidetert-butylaminedeprotectionepilepsysynthesis

曾宪烜、刘伟锋、刘地发

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江西青峰药业有限公司,江西 赣州 341000

唑尼沙胺 叔丁胺 脱保护 癫痫 合成

2024

山东化工
山东省化工研究院 山东省化工信息中心

山东化工

影响因子:0.249
ISSN:1008-021X
年,卷(期):2024.53(1)
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