丹参素及其衍生物合成方法的研究进展

中药丹参的活性成分丹参素是一种化学结构简单但特殊,并具有广泛的生理药理学活性的有机小分子化合物,丹参素类药物在抗心肌缺血和保肝护肝等方面疗效显著.然而,仅依靠从丹参中分离得到丹参素（或其衍生物）远不能满足临床需要.依靠化学方法简洁、高效的合成丹参素（或其衍生物）是该类药物研发亟须解决的问题之一.综述了近年来国内外相关报道,对外消旋体和光学纯丹参素的合成路线进行讨论,并就其构效关系进行初步分析;其中,光学纯丹参素的简单、高效、高选择性合成仍然是药物化学和有机化学关注的重点.新的合成方法和有关丹参素详细的构效关系研究,对开发丹参素类药物具有重要意义.

Advances of Synthesizing Danshensu and Its Derivatives

Danshensu, the active component of Danshen, is a kind of organic compound with simple but particular chemical structure, and widespread physiological and pharmacological activities, especially in the anti-myocardial ischemia and liver protection. However, the sources of Danshensu （or its derivatives） which are isolated from Danshen are limited and could not satisfied the clinical need. Therefore, how to synthesis Danshensu（or its derivatives） simply and effectively using chemical methods is the crucial problem needing to be solved during the process of drug development. In the essay,the relative reports in recent years were reviewed and the synthesis pathway for racemic body and optic pure danshensu were discussed, the structure-function relationship were primarily analyzed, among them, how to synthesis optic pure danshensu using simply,high effective and selective method remain to be the focus of medical chemistry and organic chemistry. The study regarding novel synthesis methods and detailed exploration of structure-function relationship would provide basis for the development of Danshensu-like drugs.