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‐1 H ‐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 deprotection were applied. Furthermore, 1‐alkoxyindole‐3‐carboxylates can be synthesized by use of the same protocol(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)