乐卡地平合成的研究进展  

Progress in the synthesis of lercanidipine

作　　者：韩艳淑[1] 刘乾才[1] 

机构地区：[1]华东师范大学化学系,上海200062

出　　处：《中国新药杂志》2008年第2期114-118,共5页Chinese Journal of New Drugs

基　　金：教育部留学回国人员基金(2004-527)

摘　　要：乐卡地平为第三代二氢吡啶类钙通道阻滞剂,主要用于高血压的治疗。作用机制与其他同类药物相似,即可逆地阻滞血管平滑肌细胞膜L型钙通道的Ca2+内流,扩张外周血管而降低血压。由于对结构进行了修饰优化,使其与其他二氢吡啶类药物相比具有高度的血管选择性、强亲脂性、短的血浆半衰期且疗效持久,不良反应发生率低,具有很好的临床应用潜力,故研究其合成具有重要意义。现综述了乐卡地平的合成研究进展,供该类新药的合成研发参考。Lercanidipine is a calcium channel blocker of the third generation dihydropyridine class used mainly as an antihypertensive medicament. Its mechanism is retarding reversibly Ca^2＋ in L-type calcium channel of vascular smooth muscle cell membranes flowing inside, and to lower blood pressure by expanding vessel. It shows high vascular selectivity, high lipophilic and short vascular half life, long duration of action, low adverse drug reaction probability compared to other drugs of the dihydropyridine class,which could have potential clinical application. Therefore,it is important to investigate its synthesis method . The recent progress in the synthesis of lercanidipine reviewed in the paper provides the reference for the research and development of this kind of new drugs.

关 键 词：1 4-二氢吡啶衍生物 合成 乐卡地平 抗高血压药物 

分 类 号：R972.4[医药卫生—药品] R914.5[医药卫生—药学]