哌库溴铵的合成工艺改进  

Improved Synthesis of Pipecuronium Bromide

作　　者：李文有[1,2] 宋园园[2] 陈宏博[2] 

机构地区：[1]酒泉职业技术学院,甘肃酒泉735000 [2]大连理工大学精细化工国家重点实验室,辽宁大连116012

出　　处：《精细化工中间体》2013年第3期35-38,44,共5页Fine Chemical Intermediates

摘　　要：以表雄酮为原料,经磺酰化、消除、溴代、环氧化、N-甲基哌嗪取代并开环、还原、酯化、成盐等反应得到哌库溴铵(必可松)。总收率达到19.32%,其结构经1H NMR和MS表征。在关键中间体2β,16β-二-(4-甲基哌嗪基)-3α-羟基-17-酮-5α-雄甾烷(5)的合成中,将其中的溴代和开环加成合并为一步,减少反应步骤,有效降低了合成成本,有利于工业生产。Pipecuronium bromide（1） was synthesized in overall yield of 19.3% in several steps and its structure was characterized with ^1H NMR and MS spectra.In the synthesis process of the key intermediate 2β,16β-bis-（4methyl-piperazinyl）-3α-hydroxy-17-keto-5α-androst steranes（5）,the bromination was combined with the ring-opening addition in one step thus effectively reduced the production costs.This improved process is simple and conducive to industrial production.

关 键 词：哌库溴铵 合成工艺 改进 

分 类 号：R914[医药卫生—药物化学]