Bridged ring systems represent long-standing targets for organic chemists because they are versatile skeletons of natural products and pharmaceuticals. Among them, saturated bicyclo[n. 1.1]alkanes have emerged as attractive synthetic targets because they are becoming ever more important in the design and development of new pharmaceuticals. For example, bicyclo[1.1.1]pentanes, 11 bicyclo[2.1.1]hexanes and bicyclo[3.1.1]heptanes are emerging benzene bioisosteres (Scheme 1A). Replacing planar benzene rings with such three-dimensional bicyclic molecules could potentially ameliorate physicochemical and pharmacokinetic properties, thereby increasing the odds of drug development success. In addition, bicyclo[n. 1.1]alkanes are widely present in natural products or as key intermediates to complex molecules (Scheme 1B). Therefore, the development of novel strategies for the synthesis of bicyclo[n. 1.1]alkanes would not only enrich the toolkit of synthetic chemists but also greatly enlarge the compound library accessible for drug discovery.