Epiberberine, a natural alkaloid derived from certain plants, has found significant application in chemical synthesis. Due to its unique structure and properties, Epiberberine is commonly employed as a building block in the synthesis of novel bioactive compounds. Its rigid tetracyclic core serves as a versatile platform for the creation of diverse chemical structures through various synthetic transformations.One key application of Epiberberine in chemical synthesis is its role as a precursor for the synthesis of berberine derivatives. By selectively modifying the functional groups present on the Epiberberine scaffold, chemists can access a wide range of berberine analogs with potentially enhanced biological activities. This approach enables the exploration of structure-activity relationships and the development of new drug candidates with improved pharmacological profiles.Additionally, Epiberberine can be utilized as a chiral building block in asymmetric synthesis. Its inherently chiral structure allows for the introduction of stereochemical diversity into target molecules, leading to the creation of enantiopure compounds of pharmaceutical interest. Through strategic manipulation of the Epiberberine framework, chemists can access complex molecular architectures with high levels of stereocontrol, enabling the synthesis of optically active compounds for various applications.Furthermore, Epiberberine has been investigated in the field of metal-catalyzed transformations. Its scaffold can serve as a ligand or substrate in metal-catalyzed reactions, facilitating the construction of C–C and C–N bonds with high efficiency and selectivity. By leveraging the unique reactivity of Epiberberine in metal-mediated processes, chemists can streamline the synthesis of intricate molecules and access valuable intermediates for further elaboration.In conclusion, Epiberberine plays a pivotal role in chemical synthesis by serving as a key intermediate for the construction of bioactive compounds, a versatile building block for enantioselective synthesis, and a valuable substrate in metal-catalyzed transformations. Its structural flexibility and synthetic utility make it a valuable tool for the design and preparation of complex molecules with potential applications in drug discovery, material science, and beyond.