盐酸安非他酮的合成研究  

Synthesis of Bupropion Hydrochloride

作　　者：何威望 沈剑锋 王玮 陶伟锋 颜平秋 席眉扬 李琰 邓莉平[1,2,3] He Weiwang;Shen Jianfeng;Wang Wei;Tao Weifeng;Yan Pingqiu;Xi Meiyang;Li Yan;Deng Liping(Department of Pharmacology,Chemistry and Chemical Engineering Institute,Shaoxing University,Shaoxing 312000,China;Shaoxing University Yuanpei College,Shaoxing University,Shaoxing 321000,China;Zhejiang Supor Pharmaceuticals,Shaoxing 312071,China)

机构地区：[1]绍兴文理学院化学化工学院药学系,浙江绍兴312000 [2]绍兴文理学院元培学院医药与健康分院,浙江绍兴312000 [3]浙江苏泊尔制药有限公司,浙江绍兴312071

出　　处：《山东化工》2020年第9期18-20,23,共4页Shandong Chemical Industry

基　　金：2019年浙江省科技厅公益性项目(GF20H300011)。

摘　　要：盐酸安非他酮(bupropion hydrochloride)主要用于戒烟,治疗抑郁症。实验中将间氯苯丙酮作为起始原料,在双氧水-氢溴酸中进行溴化反应,合成中间体3’-氯-α-溴代苯丙酮。再进行胺化反应,得到安非他酮,浓盐酸酸化后得到粗品盐酸安非他酮。最后对粗品进行重结晶,获得成品。正交实验结果显示最优方案为反应温度40℃、反应时间16 h、溶剂类型为二氯甲烷。运用IR、HNM进行结构验证。按优化条件进行实验,操作简便,回收率高,产率为79. 8%。Bupropion hydrochloride is mainly used for smoking cessation and treating depression.In the experiment,3'-Chlorophenylacetone was used as a starting material,and bromination reaction was carried out in hydrogen peroxide-hydrobromic acid to synthesize the intermediate 3'-chloro-2'-bromopropiophenone.The amination reaction is further carried out to obtain bupropion,and the crude hydrochloric acid is acidified to obtain crude bupropion hydrochloride.Finally,the crude product is recrystallized to obtain a finished product.The results of orthogonal experiments showed that the optimal scheme was reaction temperature 40℃,reaction time16 h,and the solvent type was dichloromethane.The experiment was carried out under optimized conditions with a yield of 79.8%.

关 键 词：盐酸安非他酮 间氯苯丙酮 溴化反应 

分 类 号：TQ463.24[化学工程—制药化工]