抗癌大环化合物的环合方法

Ring Closure Approaches Toward the Synthesis of Anticancer Macrocyclic Compounds

大环化合物具有广泛的生物活性。一些具有抗癌活性的天然大环化合物已开发成上市药物或应用于临床研究。在抗癌大环化合物的合成中,环合步骤是整个合成过程中的关键,同时也是难点所在。目前已经发展出了一些方便实用的环合方法。文章以具有抗癌作用的大环化合物为例,简要介绍各种常用的大环环合方法及应用。

Macrocyclic compounds continue to capture attention from academic for their diversity biological activities.Great efforts have been devoted to explore practical methods for the macro-ring cyclization,which is,in most cases,the key step in the syntheses of diverse purposes.Many useful and convenient methods or preparations have been discovered,such as the ring closure metathesis（RCM）,the Pd-catalyzed coupling reaction,the lactamization and lactonization reaction.Herein a brief review of these approaches as well as their application will be presented.