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The Copper‐Catalyzed C‐3‐Formylation of Indole CH Bonds using Tertiary Amines and Molecular Oxygen

2012; Wiley; Volume: 354; Issue: 13 Linguagem: Inglês

10.1002/adsc.201200345

1615-4169

Jianbin Chen, Bin Liu, Dongfang Liu, Shan Liu, Jiang Cheng,

Synthesis of Indole Derivatives

Abstract A copper‐catalyzed formylation reaction has been developed by employing oxygen (O 2 ) as the clean oxidant. The C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.