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盐酸西替利嗪的合成工艺改进 被引量:7

Improving on the synthesis of cetirizine dihydrochloride
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摘要 目的 :改进盐酸西替利嗪的合成。方法 :对关键的缩合反应进行了改进 ,以六水哌嗪和对氯氯苄为原料 ,经六步反应得到产品。结果 :所得产品纯度达到药用标准 ,总收率30% ,与已有工艺中最高产率相似 ,但成本降低。结论 :本合成方法工艺简单 。 Objective:To improve the synthesis of cetirizine dihydrochloride.Methods:Cetiˉrizine dihydrochloride were synthesized from piperazine hexahydrate and4-chlorobenzyl chloˉride by six steps reactions.Results:The overall yield was30%.Conclusion:The synthetic method was simple and practice in industrialize.
出处 《天津医科大学学报》 2003年第4期488-490,共3页 Journal of Tianjin Medical University
关键词 盐酸西替利嗪 合成 六步反应 Cetirizine dihydrochloride Synthesis Six-steps reaction
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  • 1[1]Baltes E, De Lannoy J, Rodriguez L. 2- [4- (diphenylmethyl) - 1- piperazinyl] acetic acids and their amides and pharmaceutical compositions[p] .Eur Pat Appl: EP58146, 1982 - 08 - 18
  • 2[2]Cossement E, Motte G, Bodson G, et al. Process for prepara tion of cetirizine, its dihydrochloride and optical isomers via hydrolysis and corresponding nitrles[p] .Brit UK Pat Appl: GB2225321, 1900 - 08- 30
  • 3[3]Cossement E, Gobert J, Bodson G Process for preparation of cetirizine and its dihydrochloride via etherification with haloacetates[p]. Brit UK Pat Appl: GB2225320, 1990 - 05 - 30

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