苯炔、喹啉及二氯甲烷三组分串联反应制备二氢喹啉衍生物

Synthesis of dihydroquinolone derivatives via three-component cascade reaction of arynes, quinolones and methylene chloride

本文研究了苯炔、喹啉及二氯甲烷三组分参与的串联反应,成功合成了一系列含氯的杂环化合物,在有机合成中具有重要的作用。实验结果表明:在室温条件下,2倍当量KF、18-C-6,喹啉和1.5倍当量的苯炔可以在二氯甲烷参与下实现该三组分串联反应,制备一系列二氢喹啉衍生物,产率在56%-86%之间。该串联反应具有反应条件温和、副反应较少、底物适应性广等优点。

In this paper, the three-component cascade reaction including aryne, quinoline and methylene chloride was developed,a series of heterocyclic compounds containing chlorine were successfully synthesized, which had an important role in organic synthesis. Quinolone reacting with 1.5 equiv aryne in methylene chloride at room temperature in the presence of 2 equiv KF and 18-C-6 gave a series of dihydroquinoline derivatives from 56% to 86% yields. The reaction has the advantages of mild reaction conditions and wide substrate adaptability.