Abstract A copper-catalyzed formylation reaction has been developed by employing oxygen (O 2) as the clean oxidant. The C [BOND] H bonds of indoles were C-3-formylated by tetramethylethylenediamine (TMEDA) and water (H 2 O; in situ formed and external added water) as the carbonyl source in moderate to good yields with good functional group tolerance. Thus, it represents a facile procedure leading to 3-formylindoles.