沙丁胺醇合成新方法研究  

A novel method for the synthesis of salbutamol

作　　者：程常君 李成 毛亚宁 胡泉源[1] CHENG Changjun;LI Cheng;MAO Yaning;HU Quanyuan(College of Chemistry and Chemical Engineering,Hubei University,Wuhan 430062,China)

机构地区：[1]湖北大学化学化工学院,湖北武汉430062

出　　处：《湖北大学学报（自然科学版）》2024年第5期739-742,F0003,共5页Journal of Hubei University：Natural Science

基　　金：校企(中国远大医药集团)合作研究项目资助。

摘　　要：对沙丁胺醇设计了新的化学合成路线并开展合成工艺研究。以对羟基苯甲醛为原料,依次经过氨甲基化反应、Wittig反应、酰化反应、溴化反应、胺化反应等5步反应得到游离的消旋沙丁胺醇。整个过程无需柱层析,通过简单的重结晶和萃取的方法即可得到纯度较高的目标产物。该创新的合成路线具有原料价廉易得、反应条件温和、操作简便的特点,经条件优化后5步反应总收率在51.3%,最终产物纯度在99%以上,具有工业化生产的潜力。A new synthetic route for chemical synthesis of salbutamol was designed,and thus the compound was prepared.p-Hydroxybenzaldehyde being used as starting material,racemic salbutamol was obtained through five steps,successively by aminomethylation,Wittig reaction,acylation,bromination and amination.Column chromatography was not required in the whole process,the target product could be obtained by simple recrystaling and extraction methods with high purity.The innovative route demonstrates the characteristics of cheap and easy availability of raw materials,mild reaction conditions and easy operation,which shows the potential value for industrial manufacturing.

关 键 词：对羟基苯甲醛 消旋沙丁胺醇 WITTIG反应 药物合成 

分 类 号：O626.26[理学—有机化学]