钩吻素子的合成研究进展

Research Progress on the Synthesis of Gelsemium

钩吻素子是草药钩吻的提取成分之一,为由6个环骈合而成的特殊笼状结构,具有镇痛、抗炎和抗肿瘤等广泛的生理活性,具备创制新型药物的重大潜能。目前,钩吻素子主要通过从植物中提取得到,如先利用溶剂浸渍法提取钩吻总碱,再通过柱层析或高速逆流色谱分离制备,这种方法耗时长、步骤繁琐,收率极低,严重制约了钩吻素子的后续研究与临床应用。由于近年来钩吻素子的需求量不断增加以及结构上的新颖性和优异的药理活性,对钩吻素子进行高效构建具有重要的意义。因此,该文对钩吻素子的合成进展进行了综述,包括半合成路线、全合成路线以及中间体骨架的合成路线,并重点分析了其不对称合成策略的难点,以期促进钩吻素子以及衍生物的合成以及相关研究的发展。

As one of the extracted components of herba buccaneum,buccaneum is a special caged structure formed by the combination of six cyclopian compounds.It has a wide range of physiological activities including analgesia,anti-inflammatory and anti-tumor,and has great potential to develop new drugs.At present,the alkaloids are mainly extracted from plants.For example,the total alkaloids are firstly extracted by solvent impregnation method,and then separated and prepared by column chromatography or high-speed countercurrent chromatography.This method is time-consuming,complicated and has a very low yield,which seriously limits the follow-up research and clinical application of the alkaloids.In recent years,due to the increasing demand for rostrin and its structural novelty and excellent pharmacological activity,it is of great significance to construct rostrin efficiently.Therefore,this paper reviews the progress of synthesis of leucogenes,including semi-synthetic route,total synthetic route and intermediate skeleton synthesis route,and focuses on the analysis of the difficulties of asymmetric synthesis strategy,in order to promote the synthesis of leucogenes and derivatives and the development of related research.