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抗过敏药盐酸奥洛他定的合成工艺研究 被引量:6

Study on the synthetic process of a novel anti-allergic agent olopatadine hydrochloride
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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。 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.
出处 《中国药物化学杂志》 CAS CSCD 2004年第6期363-364,367,共3页 Chinese Journal of Medicinal Chemistry
关键词 药物化学 制备 化学合成 盐酸奥洛他定 抗过敏 medicinal chemistry preparation chemical synthesis olopatadine hydrochloride antiallergic
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  • 1Katsujiro U,Shiro K,Hiroaki T,et al.6,11-Dihydro-11-oxodibenz[b,e]oxepinacetic acid with potent anti-inflammatory activity[J].J Med Chem,1976,19(7):941-945.
  • 2Etsuo O,Shizuo O,Hideyuki S,et al.Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives[J].J Med Chem,1992,35(11):2074-2084.

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