Department of Medicinal Chemistry, AstraZeneca R&D Montreal, 7171 Frederick-Banting, Ville Saint-Laurent (Montreal), Quebec H4S 1Z9 Canada.
Org Lett. 2010 Aug 20;12(16):3574-7. doi: 10.1021/ol101454x.
A practical and highly efficient route to the synthesis of pharmaceutically interesting quinoxalinone scaffolds is reported. The key step involves an intramolecular palladium-catalyzed N-arylation under microwave irradiation. The developed methodology tolerates a variety of bromoanilides to afford a diverse collection of bicyclic and polycyclic quinoxalinones in high yield.
本文报道了一条合成具有药用价值的喹喔啉酮类骨架的实用且高效的路线。关键步骤涉及在微波辐射下进行的分子内钯催化的 N-芳基化反应。所开发的方法学能够容忍各种溴代苯胺，从而以高产率得到多种双环和多环喹喔啉酮。
