摘要
目的改进文献合成西替利嗪的方法,优化工业生产。方法以氯苯和苯甲酰氯为原料,进行傅克酰化反应,合成出第一个反应中间体;在金属锌—氢氧化钠体系下,将羰基还原成醇羟基,再经过三氯化磷的卤置换反应,得到关键中间体;最后三步缩合反应和一步成盐反应,得到目标化合物,同时对目标化合物的精制方法进行了研究,以达到其作为医药原料药的特殊要求。结果及结论新的反应条件温和,操作简单,收率高于文献报导。适应工业化生产的要求,具有较大的产业化生产的优势。
OBJECTIVE Improving traditional synthesis method of Cetirizine Hydrochloride to optimize industrial production technique. METHODS The intermediate 1 was synthesized via the friedel-crafts reaction between chlorobenzene and benzoyl chloride. Then the carbonyl was reduced to hydroxyl under the system of zinc-NaOH. And the key intermediate was produced via the reaction with PCl3 ,and then through three steps of condensation reaction and one step of salt forming reaction the end compound was prepared. Finally the product was refined to achieve its special request for medicine raw material. RESULTS and CONCLUSION The new reaction condition was mild, easy to operate and had high production ratio. Adapted to industrialization production and had big industrial production superiority.
出处
《齐鲁药事》
2006年第5期300-302,共3页
qilu pharmaceutical affairs
关键词
盐酸西替利嗪
组胺
化学合成
Hydrochloric Cetirizine
histamine
chemical synthesis
