盐酸安非他酮的合成研究

Studies on the synthesis of bupropion hydrochloride

目的合成抗抑郁药盐酸安非他酮。方法采用氯化铜高选择性氯化3-氯苯丙酮得2-氯-(3-氯苯基)+1-丙酮,再经叔丁胺胺化、盐酸-异丙醇酸化成盐制得盐酸安非他酮。运用IR、1H-NMR、13C-NMR和MS进行结构鉴定。结果合成的盐酸安非他酮总收率为76％(以3-氯苯丙酮计)。结论本法氯代反应选择性高,操作简便,总收率较高。

Aim To synthesize bupropion hydrochloride as a treating depression agent. Method Bupropion hy-drochloride was synthesized from 3-chloropropiophenone by chlorination with cupric chloride, amination with t-BuNH2, acidification with HCl-i-PrOH. The structure of bupropion hydrochloride was confirmed by IR,1H-NMR, 13C-NMR and MS. Result The total yield of bupropion hydrochloride was 76% based on 3-chloropropiophenone. Conclusion The method is convenient, selectivity for a-chlorination is higher, and the total yield is higher.