A Comprehensive Review of Recent Synthetic Strategies and Functionalization of Amidines

ABSTRACT This review encompasses various transition‐metal‐catalyzed cross‐coupling reactions, metal‐free multi‐component reactions, cascade and domino reactions, [3+2] cycloadditions (enamine–azide), and common synthetic transformations that enable us to furnish desired functionalized amidines in moderate‐to‐good yields under sustainable conditions. Recent synthetic procedures permit the rapid construction of amidine frameworks with high diversity and complexity from easily accessible reagents and starting materials. In addition, amidine scaffolds were successfully synthesized and converted into various fused heterocyclic compounds, including quinoline, quinazoline, indole, imidazole, benzimidazole, pyrimidine, and triazoles, under mild conditions using sustainable methods. This review article comprehensively reviews synthetic strategies for amidines and their functionalization via catalysis from 2010 to 2025, offering valuable insights for synthetic and medicinal chemists engaged in amidine chemistry.