Over the past few years, significant research has been directed toward the development of new methods for synthetic efficiency and atom economical processes. Among them, the potential of transition metal-catalyzed reactions has been steadily demonstrated, as they provide a direct and selective way toward the synthesis of highly valuable products. We have been engaged in a project dedicated to the development of catalytic methods for the synthesis of bio-relevant targets. More specifically, we have been interested in asymmetric reductions such as hydrogenation and transfer hydrogenation reactions, which provide important catalytic approaches to fine chemicals. In this context, our contribution to this field is the development of novel ligands and organometallic complexes for C-H bond forming processes to access biorelevant targets. Some applications in this field will be presented.