沙丁胺醇中两种杂质的合成

摘要

目的 为加强对沙丁胺醇药物的质量控制,合成了欧洲药典中沙丁胺醇的两个杂质..方法:分别以4-羟基苯乙酮和3-甲基-4-羟基苯乙酮为起始原料,经溴化、N-苄基叔丁基胺取代,再用H2/Pd-C脱去苄基,最后用硼氢化钠还原合成目标化合物.结果与结论目标化合物结构经1 H-NMR、MS确证,合成的两种杂质可以作为沙丁胺醇药物质量控制的杂质对照品.该合成.方法:反应条件温和,原料易得,操作简单,收率高.%To improve the quality control of salbutamol, two related substances were synthesized. Starting from 4-hydroxy-acetophenone and 4-hydroxy-3-methyl-acetophenone,a convenient synthetic route was designed including bromination,substitution using N-(tert-butyl)benzylamine,deprotection of benzyl group, and reduction with NaBH4. The raw materials were cheap and easy to obtain and the reaction conditions were mild. The structures of the target compouds were verified by 1H-NMR and MS. The target compounds can be used as the reference substance of the related substances in the quality control of salbutamol.