盐酸西替利嗪的合成工艺改进

Improved synthesis of Cetirizine Hydrochloride

摘要:

本文旨在优化盐酸西替利嗪的原有合成工艺，优化后的工艺以氯苯和苯甲酰氯为起始原料，经傅克酰基化反应，羰基还原反应，羟基氯代反应，N-羟乙基哌嗪及氯乙酸钠的亲核加成反应，酸化成盐五步反应制得目标产物盐酸西替利嗪。和原有的合成路线相比，优化后的合成路线减少了一步反应，降低了原料成本，盐酸西替利嗪的总收率从原来的20.9%提高到24.87%，产物纯度在99%以上。产物结构经红外，核磁及质谱进行了表征确定。

Abstract:

This novel is aimed at optimizing and improving the synthesis route of Cetirizine Hydrochloride. The new synthesis route use chlorobenzene and benzoyl chloride as starting materials, through Friedel-crafts reaction, carbonyl reductive reaction, chlorination, nucleophilic substitution, obtained the product. Compared with the original synthesis route, this synthesis route shortened one reaction step, reduced the cost of raw materials, The total yield of Cetirizine Hydrochloride was increased from 20.9% to 24.87%. The structure of product was characterized by IR, 1H NMR and MS.