哌库溴铵的合成工艺  

Synthesis of Pipecuronium bromide

作　　者：郭建锋[1] 刘娟 郭丽[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川科瑞德凯华制药有限公司,四川成都610041

出　　处：《华西药学杂志》2009年第1期49-51,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的合成哌库溴铵并改进其工艺。方法以5α-雄甾-2-烯-17-酮为原料,通过酯化、环合、开环、还原等六步反应合成得到哌库溴铵。结果和结论通过工艺优化,使总收率由24.3%提高到44.6%,产物经1HNMR、IR、元素分析确证结构,经HPLC检测纯度>99.5%,并全检合格。优化后的工艺参数易于控制,生产工序便于操作,有利于工业化生产。OBJECTIVE To synthesize Pipecuronium Bromide and improve the synthetic process. METHODS Pipecuronium Bromide was synthesized from 6 steps 5α - androst - 2 - ene - 17 - one by esterification, cyclization , decyclization , reduction and so on obtain Pipecuronium Bromide. RESULTS and CONCLUSION The overall yield was increased from 24.3% to 44.6% by opti- mization, and chemical structure of the product was confirmed by 1HNMR. The purity of Pipecuronium Bromide was higher than 99.5% by determination using HPLC, and all items were up to standard. The optimized synthetic parameters were more regulated, and manufacture procedure was more operated and suitable for industrial production.

关 键 词：哌库溴铵 肌松药 合成 

分 类 号：R914[医药卫生—药物化学]