盐酸安非他酮溴化工艺的改进研究

Study on Improvement of Bupropion Hydrochloride Bromination Process

利用溴化钠在酸性条件下的氧化,即时生成溴素,与间氯苯丙酮发生溴代反应,经过胺化,成盐制备得到盐酸安非他酮。合成制备药物的同时,克服了原有芳烷基酮溴代反应的缺点,革除了溴素的使用危险,大幅提高了溴元素的利用率。并且设计了反应后溴元素的回收工艺,在整个制备过程中实现了溴的闭环循环。改进后的制备工艺产率达到78.5%,消除了溴的污染,减少了原料的消耗,实现药物的清洁生产,具有较高的应用价值。

By utilizing the oxidation of sodium bromide under acidic conditions, bromine is generated immediately, and a bromination reaction occurs with m-chlorophenylacetone. After amination, the salt is prepared to obtain bupropion hydrochloride. At the same time of synthesizing and preparing drugs, the shortcomings of the original aralkyl ketone bromination reaction are overcome, the danger of using bromine is eliminated, and the utilization rate of bromine element is greatly improved. And the recovery process of bromine element after the reaction is designed, and the closed-loop circulation of bromine is realized in the whole preparation process. The improved preparation process with a yield 78.5%, which eliminates the pollution of bromine, reduces the consumption of raw materials, realizes the clean production of medicines, and has higher application value.