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新型抗过敏药盐酸奥洛他定的合成工艺研究

Studies on the Synthesis of a New Antiallergic Drug Olopatadine Hydrochloride

【作者】 薛建英

【导师】 陈国良;

【作者基本信息】 沈阳药科大学 , 药物化学, 2004, 硕士

【摘要】 本文对抗过敏药的作用机理、分类、作用特点及其发展概况作了简述,对新型抗过敏药盐酸奥洛他定的合成工艺进行了研究。 本文对抗过敏药盐酸奥洛他定的合成路线进行了比较分析,以降低反应成本,简化操作为目标,选取了一条比较合理的合成路线,经七步反应,一步柱层析分离,合成了盐酸奥洛他定。并对五步反应进行了研究,降低了成本,使操作更简化,安全,总收率为4.2%。 奥洛他定的化学结构经~1H-NMR,MS及IR确证。

【Abstract】 The mechanisms and development of antiallergic drugs were briefly reviewed in this thesis, in which olopatadine hydrochloride, as a new antiallergic drug was introduced, olopatadine hydrochloride is an inhibitor of the release of histamine from the mast cell and a relatively selective histamine H1-antagonist, It is devoid of effects on alpha-adrenergic, dopamine, andmus carinic type 1 and 2 receptors. So the side-effect is small.The synthetic methods of olopatadine hydrochloride were discussed and optimized, 7-step synthetic route was chosen in the thesis. In order to decrease the cost, simplify the operating procedure, 5-step reaction conditions were investigated intensively. The total yield reached 4.2%.The structure of olopatadine was determined by 1H-NMR,MS and IR.

  • 【分类号】TQ463
  • 【被引频次】1
  • 【下载频次】745
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