Recent advances in site-selective transformations of β-enaminones transition-metal-catalyzed C-H functionalization/annulation.

β-Enaminone transformation strategies are widely employed in the synthesis of numerous biologically active drugs and natural products, highlighting their significance in medicinal chemistry. In recent years, various strategies have been developed for synthesizing several five- and six-membered heterocycles, as well as substituted polyaromatic scaffolds, which serve as crucial synthons in drug development, from β-enaminones. Among these approaches, site-selective transformations of β-enaminones C-H activation and annulation have been particularly well explored. This review summarizes the most recent literature (over the past eight years) on β-enaminone transformations for developing bioactive scaffolds through site-selective C-H bond functionalization and annulation.