中国药物化学杂志

目的对布洛芬的合成新路线进行探索和研究。方法以异丁基苯为起始原料,经傅克酰基化、WittigHorner反应、水解、Curtius重排和氧化反应合成了目标化合物布洛芬。结果与结论布洛芬的结构经MS、~1H-NMR和¹³C-NMR确证,该合成路线采用Wittig-Horner反应和Curtius重排取代Darzens缩合,反应步骤少,操作简单,条件温和,成本较低,总收率为76.4%(以异丁基苯计),可为工业化生产提供参考。

Ibuprofen is one of the most efficient non-steroidal anti-inflammatory drugs for antipyretic analgesia. A newsynthetic route has been developed after summarizing the synthetic routes reported for ibuprofen.It was synthesized in overall yield of 76. 4%( calculated from isobutyl benzene) starting from isobutyl benzene via the reactions of Friedel-Crafts acylation,Wittig-Horner reaction,hydrolysis,Curtius rearrangement and oxidation. Its structure is confirmed by MS,¹ H-NMR and ¹³C-NMR. The process is scalable for industrial production for its advantages of short period,mild reaction conditions and relatively lower cost.