A new, rapid and high-yielding method to prepare 3,4-disubstituted 2-trifluoromethylquinolines by a palladium catalyzed tandem Sonogashira-alkyne carbocyclization of beta-trifluoromethyl beta-enaminoketones with arynes is described. Moderate to excellent yields have been achieved under mild conditions. This reaction can also be expanded to the non-fluorine containing substrates. The reaction mechanism
描述了一种新的,快速且高产率的方法,该方法通过
钯催化的β-三
氟甲基β-烯胺酮与
芳烃的
钯催化串联Sonogashira-
炔烃碳环化反应来制备3,4-二取代的
2-三氟甲基喹啉。在温和的条件下,已实现中等至优异的产量。该反应也可以扩展到不含
氟的底物。还讨论了反应机理。