Synthesis of 1-Amino-1H-indole-3-carboxylates by Copper(I)-Catalyzed Intramolecular Amination of Aryl Bromides

A simple route to various N-substituted 1-amino-1H-indole-3-carboxylates by use of copper(I)-catalyzed intramolecular N-arylation has been established. For the preparation of N-monosubstituted and N-unsubstituted derivatives, the cyclization of Boc-protected enehydrazines and subsequent de-protection were applied. Furthermore, 1-alkoxyindole-3carboxylates can be synthesized by use of the same protocol ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)