Oxysporone, possessing a 4H-furo(2,3-b)pyran-2(3H)-one structure, is a fungal metabolite, first isolated from Fusarium oxysporum. Later, this compound was also reported from the fungal genera, Diplodia, Pestalotia and Pestalotiopsis. Oxysporone was patented as an antibiotic for the treatment of dysentery, and its phytotoxic property has been well-established. Interesting biological and chemical properties of oxysporone make this compound attractive for its potential biotechnological applications in agriculture, especially as a new agrochemical with a lower environmental impact. However, it requires further extensive bioactivity screening looking at beyond its established phytotoxicity and preliminary antifungal property. It has a simple chemical structure (C₇H₈O₄), and the hydroxyl group at C-4 provides options for synthesising numerous analogues by simply incorporating various functionalities at C-4, whilst keeping the main skeleton intact. This mini-review provides a critical overview on the occurrence, production, synthesis, structure elucidation and bioactivities of oxysporone.