Within the last few years, a significant contribution to the discovery of sp2C−H activation processes and useful applications for cross-coupling C−C bond formation has been achieved by the use of ruthenium(II) arene catalysts. The aim of this thesis is to describe a modular approach for the synthesis of several ruthenium(II) arene complexes with the potential for C−H activation. Another cutting-edge field, catalytic enantioselective functionalization of C−H bonds by transitional metal catalysts, has also been realized within the last few years. It represents a highly atom- and step-economic approach toward the generation of structural complexity. However, the majority of current methodologies rely on the usage of late third- row transition metals such as pallidum, iridium and rhodium. There is a need that motivates the search for cheaper, relative earth abundant metals that could have similar catalytic ability. Herein is also represented a preliminary study of a ruthenium(II)-catalyzed enantioselective access to chromane moiety enabled by chiral transient directing group.