文献类型：期刊文献

中文题名：盐酸安非他酮的合成研究

英文题名：Synthesis of Bupropion Hydrochloride

作者：何威望[1];沈剑锋[3];王玮[2,3];陶伟锋[3];颜平秋[3];席眉扬[1];李琰[1];邓莉平[1,2,3]

机构：[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

年份：2020

卷号：49

期号：9

起止页码：18

中文期刊名：山东化工

外文期刊名：Shandong Chemical Industry

基金：2019年浙江省科技厅公益性项目(GF20H300011)。

语种：中文

中文关键词：盐酸安非他酮;间氯苯丙酮;溴化反应

外文关键词：bupropion hydrochloride;3'-chlorophenylacetone;bromination reaction

中文摘要：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%。

外文摘要：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%.