Abstract Indole‐based molecules represent a class of organic compounds that have attracted significant attention due to their remarkable chemical properties. Among these, 3‐cyano indole is a highly valuable precursor in organic synthesis. Incorporating a cyano group into the indole ring opens new pathways for synthesizing a diverse range of functionalized indole derivatives. Furthermore, the 3‐cyano indoles core also exists in many biologically interesting compounds, attracting and inspiring scientists and researchers to develop novel methodologies with unique functional group diversification around the 3‐cyano indole to actively pursue the discovery of innovative methods capable of making a significant impact in the preparation of therapeutic agents for drug discoveries and development.