Abstract The development of novel methodologies that enable the construction of complex chiral molecular scaffolds in an atom and step‐economic manner has always been an area of immense interest and significant synthetic value. The transition metal‐catalyzed enantioselective sp 3 C−H activation and functionalization reactions serve as an expeditious means for introducing diverse functionalities in a straightforward manner. However, controlling the chemo‐ and stereoselectivity of these reactions is a significant challenge owing to their ubiquity and low reactivity. In this review, we present a comprehensive account on the recent advances in inter‐ and intramolecular asymmetric sp 3 C−H bond functionalization utilizing ruthenium, rhodium, and iridium catalysts and get insights into the mechanistic aspects of these transformations.