Selective carbon-carbon and carbon-heteroatom bond formation reactions are among the most important processes in organic chemistry since it enables the construction of common organic molecules from simple precursors. Among various methodologies, the transition metal-catalyzed transient directing group-enabled C−H functionalization process represents one of the most efficient and straightforward approaches due to the avoidance of pre-functionalization of the reaction precursors. In comparison with the well-established sp2 C−H functionalization process, much less progress has been made to the unactivated sp3 carbons with the transient directing group strategy. In view of the prevalent presence of sp3 C−H bonds in organic molecules, advances in this area will allow for broad applicability by providing a powerful and valuable synthetic approach to access common organic frameworks, such as (hetero)cycles, privileged structures in medicines. This area will be advanced further by the development of site- and enantio-selective functionalization of unactivated sp3 C−H bonds. Furthermore, demonstration of these transformations through different reaction pathways will provide a new opportunity for the design of novel transition metal-catalyzed coupling reactions on sp3 carbons. Herein, we are presenting our studies on transition metal-catalyzed transient directing group-enabled C−H functionalization reaction.
• This study could potentially be used for others to build small molecules in an efficient way.
• This study could potentially be used for others to carry out late-stage functionalization of natural products or drug molecules.
• This research could also be used by others to expand their research.