盐酸布替萘芬的合成工艺改进

摘要

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,1H-NMR and IR. Conclusion The route is simple, and can be suitable for industrial production.%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。