Recent advances in the synthesis of imidazo[2,1-a]isoquinolines and their core-embedded heterocycles.

Abstract

Imidazo[2,1-a]isoquinolines and their embedded heterocycles are a class of widely explored fused nitrogen-containing heterocyclic skeletons. These compounds are widely distributed in natural products and pharmaceutically active molecules, exhibiting diverse bioactivities such as antitumor, anti-HIV-1, antimicrobial, and enzyme inhibitory activities, which have attracted extensive attention from synthetic organic and medicinal chemists. In recent years, significant progress has been made in the synthesis of imidazo[2,1-a]isoquinolines, with various efficient and green synthetic strategies being developed, including transition metal catalysis, visible light photocatalysis, metal-free cyclization, and multi-component reactions. Based on the core strategy of constructing the heterocyclic skeleton, the reported synthetic methods can be broadly classified into three categories: imidazole ring formation, isoquinoline ring formation, and de novo formation of both imidazole and isoquinoline rings. This review systematically summarizes the recent advances in the synthesis of imidazo[2,1-a]isoquinolines, focuses on the reaction mechanisms, advantages, limitations, and substrate scopes of various synthetic methods, and briefly discusses the future development trends, aiming to provide comprehensive references for the further research and application of this class of heterocyclic compounds.

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