【作者】 王振；

【导师】 刘新泳；

【作者基本信息】 山东大学 ， 制药工程（专业学位）， 2013， 硕士

【摘要】 我国中草药历经几千年医疗实践的验证,疗效确切。然而这些药物普遍存在特异性差、毒副作用大的缺陷,因此以中草药有效成分为先导化合物开发高效、低毒的心脑血管药物是目前热点问题。川芎嗪是中药川芎的根茎中的主要药效成分,目前在临床上广泛用于心脑血管疾病的治疗,但川芎嗪生物利用度低,代谢快,半衰期短,多次给药易致毒副作用。川芎醇阿魏酸酯是以川芎嗪为先导物,开发的具有良好抗心脑血管疾病活性的候选药物。本论文在本课题组的研究基础上,对川芎醇阿魏酸酯的合成工艺进行了优化和系统的研究,确定以川芎醇为原料合成川芎醇阿魏酸酯的最佳反应步骤和反应条件,节约了成本,增加了经济效益,减少了环境污染。更多还原

【Abstract】 Chinese herbal medicines have verified effectiveness after thousands of years of medical practice. However, these drugs have the disadvantages of poor specificity and adverse effects. Consequently, development of cardiovascular drugs with high efficiency and low toxicity using the effective components in Chinese herbal medicine as lead compounds are hot issues currently.Ligustrazine as the main active component in Rhizoma Chuanxiong rhizome has been widely used in the clinical treatment of cardiovascular and cerebrovascular diseases. However, Ligustrazine has low bioavailability, fast metabolism, short half-life and adverse effects caused by repeated administration.Rhizoma Chuanxiong ferulic acid ester has been developed as a drug candidate using Ligustrazine as lead compound with good anticerebrocardiac vascular acitivity. Based on the studies in our lab, this thesis focused on the systematic optimization of the technical process on the synthesis of Rhizoma Chuanxiong ferulic acid ester, and confirmed the optimized reaction procedures and conditions for synthesizing Rhizoma Chuanxiong ferulic acid ester with Ligustrazine as starting material, thus saving the cost, increasing economic benefits and reducing the pollution of the environment.更多还原