Abstract

The synthesis of tetrahydro-?-carbolines (TH?Cs) framework is a fundamental aspect of medicinal chemistry due to their significant pharmacological applications. Herein, we developed a microwave-assisted novel approach for the synthesis of TH?C scaffolds utilizing ferrous(II) chloride as an earth abundant metal catalyst and methanol used as valuable methylene source. This methodology demonstrates excellent functional group tolerance and provides N2-substituted TH?Cs in good to excellent yields. Overall, this study highlights a sustainable and practical strategy for the synthesis of biologically important TH?Cs, thereby offering promising prospects in the drug discovery and development. © 2024 Wiley-VCH GmbH.