The development of existing and invention of new synthetic methodologies in recent years has greatly facilitated the preparation of molecules that would once have been considered an insurmountable synthetic challenge. Over the past four decades, the synthetic community has witnessed a tremendous upsurge in the field of transition metal-catalyzed C–C and C–Heteroatom bond forming reactions. The field of C(sp2)–H bond functionalization has grown rapidly over the past decade, providing many new and efficient routes for the synthesis of desirable compounds and a plethora of literature is available including a large number of reviews. In contrast, there are only a handful of reports in the literature where C(sp3)–H bond functionalization is efficiently achieved and field remains largely untouched regarding the development of new and efficient methodologies. However, despite the advances in the field of enantioselective reactions, the use of transition metal catalysts with appropriate and effective chiral ligands is still in its infancy. The overall aim of this project is to develop new chemistry to functionalize the beta-carbon of simple heterocyclic compounds like pyrrolidine and piperidine in enantioselective fashion. Finally we will apply the newly developed catalytic enantioselective C–H functionalization in bioactive natural product/drug molecule synthesis.