盐酸阿比朵尔合成工艺研究  

Study on Synthesis Process of Arbidol Hydrochloride

作　　者：马雪莲 江银枝[1] 陶寅松 MA Xuelian;JIANG Yinzhi;TAO Yinsong(School of Chemistry and Chemical Engineering,Zhejiang Sci-Tech University,Hangzhou,Zhejiang 310000,China)

机构地区：[1]浙江理工大学化学与化工学院,浙江杭州310000

出　　处：《浙江化工》2024年第10期31-37,44,共8页Zhejiang Chemical Industry

基　　金：浙江省一流课程(2020sylxs001);浙江理工大学一流课程(XXKC2201);浙江理工大学教学改革(Jgxy2022208)。

摘　　要：目的:开发绿色、经济、环保的盐酸阿比朵尔的合成工艺路线。方法:以廉价易得的乙酰乙酸乙酯为原料,经Nenitzescu反应、酰化保护酚羟基、溴化、苯硫酚化、Mannich反应、盐酸成盐6步反应得到盐酸阿比朵尔。考察物料摩尔比、催化剂、温度、溶剂等因素对反应的影响,采用HPLC确定中间体和产物纯度,LC-MS、1H NMR确定结构。结果:经优化后的盐酸阿比朵尔的总收率为44.2%,HPLC纯度为99.8%。结论:该合成工艺路线具有原料易得、条件温和、操作简单等优点,可以显著降低生产成本和减少环境污染,适合大规模工业化生产。Objective:To develop a green,economical and environmentally friendly synthetic route of arbidol hydrochloride.Methods:Arbidol hydrochloride was obtained by using cheap and easily available ethyl acetoacetate as raw material,and was subjected to 6 steps of Nenitzescu reaction,acylation of protective phenol hydroxyl reaction,bromination reaction,phenylthiophenolation reaction,Mannich reaction,and hydrochloric acid salting reaction.The effects of molar ratio,catalyst,temperature,solvent and other factors on the reaction were investigated,and the purity of intermediates and products was determined by HPLC,and the structure was determined by LC-MS and'H NMR.Results:The optimized total yield of arbidol hydrochloride was 44.2%and the HPLC purity was 99.8%.Conclusion:The synthesis route has the advantages of easy availability of raw materials,mild conditions and simple operation,which can significantly reduce production costs and environmental pollution,and is suitable for large-scale industrial production.

关 键 词：盐酸阿比朵尔 抗流感病毒 合成 工艺优化 表征分析 

分 类 号：TQ460.6[化学工程—制药化工]