盐酸屈他维林中间体3,4-二乙氧基苯乙胺合成工艺的改进  

Improvement of Synthesis Process of Drotaverine Hydrochloride Intermediate 3,4-Diethoxyphenethylamine

作　　者：董鑫 刘苏毅 姜军 王凯[1] DONG Xin;LIU Suyi;JIANG Jun;WANG Kai(College of Health Science and Engineering,Hubei University,Wuhan 430062,China)

机构地区：[1]湖北大学健康科学与工程学院,湖北武汉430062

出　　处：《武汉工程大学学报》2023年第3期272-275,共4页Journal of Wuhan Institute of Technology

基　　金：湖北省功能化学品工程技术研究中心开放基金(GCZX-2022-07)。

摘　　要：盐酸屈他维林是一种应用广泛的平滑肌解痉类药物,对其工业化生产工艺的研究具有现实意义。盐酸屈他维林中间体3,4-二乙氧基苯乙胺的现有工业化路线存在一些问题,包括氰化物的使用,高温高压等危险反应。在遵循安全环保的前提下,对其传统合成路线进行改进,以廉价易得的邻苯二酚为原料,经过傅克酰基化、乙基化、Gabriel胺合成和黄鸣龙还原四步反应得到3,4-二乙氧基苯乙胺。该合成方法规避了易燃易爆物质及贵金属催化剂的使用,后处理简单,生产成本低,总收率为66.2%,在工业化生产中具有突出优势。Drotaverine hydrochloride is widely used as an antispasmodic drug for smoothing muscle.It is of practical significance to study its industrial production technology.There are some problems in the existing industrialized route of drotaverine hydrochloride intermediate 3,4-diethoxyphenethylamine,including the use of cyanide,dangerous reaction conditions such as high temperature and high pressure.Under the premise of safety and environmental protection,the traditional synthetic route was improved in this paper.3,4-Diethoxy-phenethylamine was obtained with cheap and easily available starting material catechol through four steps of Friedel-Crafts acylation,ethylation,Gabriel amine synthesis and Huang Min-long reduction.The synthetic method avoids the use of flammable and explosive substances and noble metal catalysts,and has simple post-treatment and low production cost,with a total yield of 66.2%,which has outstanding advantages in industrial production.

关 键 词：盐酸屈他维林 3 4-二乙氧基苯乙胺 工艺改进 

分 类 号：O626.13[理学—有机化学]