Development of Synthetic Methods for HeterocyclesUsing Palladium-Catalyzed C-H Functionalization

开发了一种新的催化合成4-芳基-2-喹诺酮类化合物的方法，该方法包括两个机械独立的、由钯催化的连续反应--氧化Heck反应和分子内C-H酰胺化--这两个反应都在一个基于钯的催化体系中顺利进行。此外，还发现水可以作为反应介质成功地用于钯催化的硫代苯甲胺的C-H环化反应。反应在较温和的水中进行，为2-芳基苯并噻唑的合成提供了一种更实用、更环保的方法。

A novel catalytic method for synthesizing 4-aryl-2-quinolinones was developed that involves two mechanistically independent, sequential palladium-catalyzed reactions-the oxidative Heck reaction and the intramolecular C-H amidation-both of which smoothly proceeded in the presence of a single, palladium-based catalytic system. In addition, it was found that water can be successfully employed as a reaction medium in palladium-catalyzed C-H cyclization of thiobenzanilides. Reactions efficiently proceeded under considerably mild conditions in water, providing a more practical, greener method for the synthesis of 2-arylbenzothiazoles.