One-Pot Synthesis of N-Fused Benzimidazo-β-carbolines through Sequential Propargylation/ aza-Cycloisomerization Approach

J Org Chem. 2024 Feb 16;89(4):2675-2682. doi: 10.1021/acs.joc.3c02702. Epub 2024 Feb 6.

Abstract

The first sequential acid-catalyzed propargylation/base-mediated aza-cycloisomerization between indolyl-benzimidazoles and propargylic alcohols is described. This protocol enables the one-pot construction of N-fused benzimidazo-β-carbolines in good yields. The synthetic utility of this approach is demonstrated by the assembly of an aza-helicene and also by a gram-scale reaction.