CH Functionalization‐Based Strategy in the Synthesis and Late‐Stage Modification of Drug and Bioactive Molecules

Abstract

Abstract CH functionalization approach is an attractive strategy in synthetic chemistry for the construction and diversification of bioactive drug molecules and their developments. Transition metal‐catalyzed CH activation, Minisci type radical reaction, and metal/organo‐photoredox‐catalyzed reactions are the hottest approaches, used in the organic chemist's toolbox for the rapid construction and late‐stage modification of functionalized bioactive scaffolds to achieve the desired drug research and development. In this aspect, the de novo synthesis has been utilized for the formation of drug molecules having new carbon–carbon and carbon–hetero bonds more efficiently within fewer steps via CH functionalization reactions. On the other hand, late‐stage functionalization is studied for the fast construction of highly diversified drug scaffolds without any kind of prefunctionalizations and has a major impact on drug discovery. In this article, we focus on the significant advances achieved in the CH functionalization‐based strategies including late‐stage methodology for the synthesis of selective drugs and drug‐like compounds found in academia as well as industry and showcase how the implementation of these modern strategies successfully accelerate the selectivity and efficiency in the drug discovery process to access new molecules of interest.