Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China.
Chem Commun (Camb). 2010 Mar 28;46(12):2145-7. doi: 10.1039/b925285a. Epub 2010 Feb 25.
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 is also discussed.
一种新的、快速高产的方法,通过钯催化的β-三氟甲基β-烯胺酮与芳炔的串联 Sonogashira-炔烃环化反应来制备 3,4-二取代的 2-三氟甲基喹啉。在温和的条件下,中等至优异的产率已经实现。该反应也可以扩展到非含氟的底物。还讨论了反应机理。