Development of new synthetic methodologies plays an irreplaceable role in the synthesis of natural products anddesigned bioactive molecules.On the other hand,the structures of the synthetic targets can shed a light on discovery ofnew reactions and synthetic strategies.In this lecture we will describe our recent progress in Cu-catalyzed arylationwith aryl chlorides1 and Rh-catalyzed regioselective functionalization at C-7 position of protected indoles.2 The drivingforce for developing these new methodologies is to meet the requirement in our studies on target synthesis.