Executive Summary : | Devising catalytic synthetic strategies for the production of useful organic molecules including natural products, privileged scaffolds, and drug candidates in an environmentally benign manner is a forefront area of research in chemical science. In this realm, the transition-metal-catalyzed functionalization of C-H bond has attracted the synthetic community owing to its ease in building molecular complexity from simple starting materials and efficiency in the late-stage functionalization of biologically significant molecules. The fundamental step in this strategic endeavor is the facile and selective generation of metallacycle, the pivotal organometallic intermediate that governs the desired functionalization. In this proposal, new reactivity concepts and catalytic strategies to access metallacycles and their reactions leading to the synthesis of a wide range of pharmaceutically significant molecules have been portrayed. The innovation phase focuses on metallacycle generation through the activation of C-H, C-C, and C=C bonds, and the application phase depicts the synthetic utilities of the proposed strategies. Synthesis and functionalization protocols of relatively unexplored biaryl frameworks will be explored with a specific focus on asymmetric functionalization providing molecules with point chirality as well as axial chirality. It is worth noting that modern drugs are needed in enantiomerically pure form and the current era of drug designing platforms will be benefited from these developments. Further, the concept of nucleometalation has also been sketched toward challenging alkene functionalization, and the merger of transition-metal-catalyzed C-H/C-C activation is planned to prepare indole-based alkaloids natural products. Overall, the proposal demonstrates new reaction modalities which will not only advance the fundamentals of organic synthesis but also contribute to the development of new exciting research areas. |