H BOND ACTIVATION;
ANTAGONISTS;
POTENT;
FUNCTIONALIZATION;
ALKENYLATION;
QUINOLINES;
INHIBITORS;
DISCOVERY;
PYRIDINES;
D O I:
10.1021/ol900103a
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
A method for the direct arylation of benzotriazepines is reported, employing an aryl iodide as the coupling partner, copper iodide as the catalyst, and lithium tert-butoxide as the base. A variety of electron-rich, electron-poor, and sterically hindered aryl iodides are compatible with the reaction conditions. The arylation reaction can also be performed outside a glovebox in air without a significant decrease in yield. Furthermore, convenient microwave conditions for carrying out this transformation are reported.