Microwave-assisted, Pd-catalyzed one-pot synthesis of δ-carbolines through demethylative amine arylation

The rarely explored N-demethylative functionalization of tertiary amines enables the creation of a variety of complex motifs in a distinctive pathway. In this context, we demonstrate a domino protocol for the synthesis of δ-carbolines from tertiary amines via a Suzuki and N-demethylative arylation sequence. This one-pot method is straightforward to operate under microwave conditions, and the easily accessible starting materials enhance the robustness of the methodology. This Pd-catalyzed, ligand-free strategy sheds light on the arylation reaction of tertiary amines using 2-fluorophenylboronic acids.