Nitrogen-based heterocycles are an important class of structural scaffolds distributed in biologically active natural products, medicinal chemistry, and agrochemicals. Hence, there is increasing interest in the development of novel synthetic strategies for the construction of these privileged structural motifs. Recently, 3-aminoindazoles have emerged as versatile synthons participating in a variety of condensation annulation, denitrogenative transannulation and rearrangement ring expansion reactions, which provide efficient synthetic routes for the formation of nitrogen heterocycles. This review systematically highlights for the first time the most recent advances in 3-aminoindazoles to provide a deep understanding of using 3-aminoindazoles as versatile synthons in organic transformations for synthetic and medicinal chemists.