Practical synthesis of quinoxalinones via palladium-catalyzed intramolecular N-arylations.
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.
Luo
Xuehong
X
Department of Medicinal Chemistry, AstraZeneca R&D Montreal, 7171 Frederick-Banting, Ville Saint-Laurent (Montreal), Quebec H4S 1Z9 Canada. xuehong.luo@astrazeneca.com
Chenard
Etienne
E
Martens
Peter
P
Cheng
Yun-Xing
YX
Tomaszewski
Mirosław J
MJ
D002384:Catalysis; D020650:Combinatorial Chemistry Techniques; D003500:Cyclization; D008872:Microwaves; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry
D011810:Quinoxalines; D010165:Palladium