盐酸安非他酮杂质F的合成和表征

Preparation of Bupropion Hydrochloride Impurity F

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.