Synthesis of Benzazepinoindole Derivatives via a One‐Pot Process of TiCl₄‐Catalyzed Indole Alkylation/Pictet‐Spengler Cyclization

Abstract

An efficient synthetic approach involving indole alkylation/Pictet-Spengler cyclization was developed to form benzazepinoindole derivatives. The reactions proceeded smoothly with indoles, 2-aminobenzyl alcohols, and aldehydes in the presence of TiCl 4 as a Lewis acid catalyst. The developed one-pot protocol is operationally simple and tolerates various functional groups. Furthermore, this mild and practical tandem reaction provides a direct route to access benzazepinoindole-containing natural products and bioactive compounds.[a] E.