Efficient Synthesis of β‐Carboline–Tetrazole Frameworks via Ugi–Azide Multicomponent Reaction

ABSTRACT The development of structurally diverse heterocyclic hybrids with potential biological activity remains a cornerstone of modern medicinal chemistry. In this study, we provide a comprehensive summary of recent research developments of β‐carboline and the design and synthesis of its derivatives using a one‐pot four‐component Ugi reaction. In the Ugi–azide reaction, the carboxylic acid component is replaced by an azide, enabling the formation of peptidomimetic compounds. These novel β‐carboline‐based heterocyclic hybrids hold promise for applications in medicinal chemistry and drug discovery. Furthermore, the Ugi–azide reaction aligns with the principles of green chemistry, offering an atom‐economic, waste‐minimizing approach that optimizes resource utilization. This work highlights the versatility of the Ugi–azide reaction in synthesizing bioactive compounds and its potential contribution to sustainable chemical synthesis.