Simple Modular Synthesis of Substituted Pyridines

Significance

A new method for Cu-catalyzed C-N bond formation is developed. Using it, an elegant reaction cascade starting from easily available materials allows a versatile modular synthesis of polysubstituted pyridines. The reaction is especially suitable for the preparation of pyridines bearing several aryl or heteroaryl substituents. It can be used as well to access functionalized azaphenantrenes and similar polycyclic systems. Such compounds represent significant interest for medicinal chemistry and drug design.