Advances in Metal‐Catalyzed Buchwald–Hartwig Coupling for Bioactive Molecule Synthesis: A Review

ABSTRACT Metal‐catalyzed cross‐coupling reactions that form C–N bonds have become valuable methods for constructing various heterocyclic systems. The Buchwald–Hartwig amination reaction of aryl halides has attracted considerable attention in recent years for the synthesis of (hetero)arylamines, which are fundamental structures in natural products, medicines, and other physiologically active compounds. Our purpose here is to provide readers with information about recent advances in this strategy for C‐N bond formation, particularly in the construction of various heterocyclic systems. This review examines developments in Buchwald–Hartwig coupling for the synthesis of bioactive molecules from 2014 to the present.