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抗过敏药盐酸奥洛他定的合成工艺研究
Study on the synthetic process of a novel anti-allergic agent olopatadine hydrochloride
【摘要】 目的合成新型抗过敏药盐酸奥洛他定。方法以对羟基苯乙酸和苯酞为原料 ,经亲核取代、脱水环合、Wittig反应、成盐制备盐酸奥洛他定。结果目标化合物的结构经氢谱、质谱确证 ,总收率约 5 9%。结论改进了合成路线 ,为进一步工业生产和临床应用打下基础。
【Abstract】 Aim To synthesize a novel anti allergic agent olopatadine hydrochloride.Methods Starting from the starting material 4 hydroxyphenylacetic acid.Olopatadine hydrochloride was synthesized via nucleophilic substitution,cyclization,Wittig reaction,salt formation.Results The structure of the target compound was confirmed by MS, 1H NMR,the overall yield was 5.9%.Conclusions The synthetic process of olopatadine hydrochloride is improved and suitable for industrial manufacture.
【关键词】 药物化学;
制备;
化学合成;
盐酸奥洛他定;
抗过敏;
【Key words】 medicinal chemistry; preparation; chemical synthesis; olopatadine hydrochloride; antiallergic;
【Key words】 medicinal chemistry; preparation; chemical synthesis; olopatadine hydrochloride; antiallergic;
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2004年06期
- 【分类号】TQ463
- 【被引频次】7
- 【下载频次】728