盐酸安非他酮杂质F的合成和表征  

Preparation of Bupropion Hydrochloride Impurity F

作　　者：胡克斌 谭跃浪 瞿春艳 吴寒梅 胡明阳 邹志锋 HU Ke-bin;TAN Yue-lang;QU Chun-yan;WU Han-mei;HU Ming-yang;ZOU Zhi-feng(Zhejiang Apeloa Jiayuan Pharmaceutical Co.,Ltd.,Dongyang 322118,China;Zhejiang Apeloatospo Pharmaceutical Co.,Ltd.,Dongyang 322118,China;Apeloa Pharmaceutical Co.,Ltd.,Dongyang 322118,China)

机构地区：[1]浙江普洛家园药业有限公司,浙江东阳322118 [2]浙江普洛得邦制药有限公司,浙江东阳322118 [3]普洛药业股份有限公司,浙江东阳322118

出　　处：《精细化工中间体》2022年第6期42-45,89,共5页Fine Chemical Intermediates

摘　　要：以盐酸安非他酮中间体溴化物2-溴-3’-氯苯丙酮(4)为原料,先水解成1-(3-氯苯基)-2-羟基-1-丙酮(3),再氧化成1-(3-氯苯基)丙烷-1,2-二酮(2),再经还原,得到安非他酮杂质F。其结构经MS和NMR表征确证。该合成路线的原料易得,反应条件温和,反应选择性好,后处理的分离纯化操作简便易行,能够制得高纯度的安非他酮杂质,为安非他酮杂质F提供基础。The bromides of bupropion hydrochloride 2-bromo-3’-chloropropiophenone(4)were hydrolyzed to give 1-(3-chlorophenyl)-2-hydroxy-1-acetone(3),then oxidized to obtain 1-(3-chlorophenyl)propane-1,2-dione(2),after selective reduction with suitable reducing agent,the impurity F of bupropion was obtained The raw materials used in the whole synthetic route are easy to obtain,the reaction conditions are mild,the reaction selectivity is good,and the separation and purification operation of post-processing is simple and easy,which can produce high-purity bupropion impurities,so it is suitable for use as the impurity reference substance of bupropion.

关 键 词：抗抑郁药 安非他酮 选择性还原 

分 类 号：TQ463.24[化学工程—制药化工]