The catalytic activation of carbon-carbon single bonds is a major challenge in organometallic chemistry, since the lack of prefunctionalization steps opens the way to new, economically and ecologically attractive reaction pathways. Strained ring substrates occupy a privileged role in C-C bond activations as the release of their ring strain facilitates the desired metal insertion. Important progress has been made in the field in the last decade. However, the development of asymmetric versions lags behind. This thesis shows the development of new methodologies for the enantioselective C-C bond activation of cyclobutane derivatives.