With conditions for the Pd(0)-catalyzed C-N bond-forming step established, the optimization of the one-pot process was explored (Table ). The optimal ligand/base pairing of HPCy3BF4 with K3PO4 was identified, which formed 9a from 1a and 6a in 78% yield. This highlights that the second C-H activation step is regioselective for the 7-position of 6a.