盐酸去甲乌药碱的合成及产业化  

Synthesis and Industrialization of Noraconitine Hydrochloride

作　　者：胡美华 成新华 程杰明 袁欣 靳月莎 HU Mei-hua;CHENG Xin-hua;CHENG Jie-ming;YUAN Xin;JIN Yue-sha(Hunan Sanqing Pharmaceutical Co.,Ltd.,Hunan Changsha 410031,China)

机构地区：[1]湖南三清制药有限公司,湖南长沙410031

出　　处：《广州化工》2024年第11期154-156,共3页GuangZhou Chemical Industry

摘　　要：以(4-羟基-苯基)-乙酸为起始原料,先还原为醇再氧化为醛,然后与2-(3,4-二羟基苯基)乙胺发生Pictet-Spengler反应,便得到去甲乌药碱;精制后得到高纯度的目标化合物。该工艺原料易得,操作便捷,且绿色环保,适合产业化生产,总收率达42.2%,含量99.5%。本文还介绍了我们公司质检部门利用高效液相色谱检测盐酸去甲乌药碱的含量,包括溶液配制、样品前处理、液相色谱条件、进样和计算等,从而得到样品的含量。讨论了该工艺涉及两步重要的反应,Pictet-Spengler反应和活化DMSO氧化醇的反应。With(4-hydroxy-phenyl)-acetic acid as the starting material,it was reduced to alcohol then oxidized to aldehyde.Then Pictet Spengler reaction occured with 2-(3,4-dihydroxyphenyl)ethylamine.It was obtained high-purity target compounds through refinement.The process had the advantages of easy availability of raw materials,convenient operation and environmental protection.It was suitable for industrial production with a total yield of 42.2%,the content was 99.5%.The use of high-performance liquid chromatography by the quality control department of our company to determine the content of norepinephrine hydrochloride was also introduced,including solution preparation,sample pretreatment,liquid chromatography conditions,sampling and calculation,so as to obtain the sample content.Two important reactions,Pictet-Spengler reaction and activation of DMSO to oxidize alcohols,were discussed.

关 键 词：合成 Pictet-Spengler反应 去甲乌药碱 产业化 

分 类 号：R914.5[医药卫生—药物化学]