Synthesis of 2‐Amino‐3‐arylindoles and their Fused Analogues via Intramolecular C‐Arylation
Kateřina Žáková,
Petra Králová,
Miroslav Soural
Abstract:2‐Aminobenzyl cyanide was reacted with nitrobenzenesulfonyl chlorides and alkylated under Mitsunobu or Fukuyama conditions. The resulting intermediates were exposed to basic conditions, which triggered a Truce‐Smiles rearrangement, leading to intramolecular C‐arylation. This reaction was followed by spontaneous cycloaddition, which yielded 2‐aminoindole derivatives. The developed synthetic route represents a simple and metal‐free approach for accessing 1‐substituted 2‐amino‐3‐arylindoles. Furthermore, pyrimido… Show more
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