In order to overcome hypoxia-related limitations, the design and development of biocompatible molecular vectors able to deliver O2 directly to the target tissues is gaining significant attention in the pharmacological field. In this context, an increasing amount of literature focused on aromatic endoperoxides (EPOs) as suitable Oxygen-Releasing Agents (ORAs). The polycyclic aromatic precursors are cheap, versatile substrates able to reversibly bind and release O2 when properly functionalized and stimulated. The chemistry of these interesting EPOs has been deepened in the past and many aspects regarding their preparation and reactivity are now well-known and established. Among others, the group of W. Fudickar and T. Linker was able to produce a remarkable amount of EPOs from both anthracene and naphthalene derivatives.