盐酸布替萘芬的合成工艺改进  

Improved synthesis of Butenafine Hydrochloride

作　　者：李新志 杨传伟 徐传彬 刘杰 许敏 吴世德 

机构地区：[1]山东明仁福瑞达制药股份有限公司山东省骨科疼痛类药物工程研究中心,山东济南250104

出　　处：《食品与药品》2016年第6期401-403,共3页Food and Drug

摘　　要：目的：改进盐酸布替萘芬的合成工艺。方法以萘为起始原料，经氯甲基化反应制得1-氯甲基萘，再被甲胺取代得到关键中间体N-甲基-1-萘甲胺盐酸盐，后与对叔丁基氯苄缩合，经成盐、重结晶得到盐酸布替萘芬精制品。结果盐酸布替萘芬合成总收率为45.5%，纯度99.88%，所得产品经质谱（MS）、核磁共振氢谱（1H-NMR）和红外光谱（IR）确证。结论改进后的工艺操作简单，适合工业化生产。Objective To improve the synthesis process of butenafine hydrochloride.MethodsButenafine hydrochloride was synthesized from naphthalene by chloro-methylation reaction, substitution reaction, condensation with 4-tert butyl benzyl chloride and salification, then was purified by recrystallization. Results The total yield was 45.5 %, and the purity was 99.88 %. The structure of target compound was confirmed by MS,1^H-NMR and IR. Conclusion The route is simple, and can be suitable for industrial production.

关 键 词：盐酸布替萘芬 氯甲基化 对叔丁基氯苄 合成 

分 类 号：R914.5[医药卫生—药物化学]