Xyloketals, unique bioactive compounds, isolated from mangrove fungus Xylaria sp. (no. 2508), having multiple pharmacological, therapeutic properties, have prompted enormous research on their stereochemistry, bioactivity and synthetic attempts made toward this novel family. This review brings forward a systematic and comprehensive survey of the method of both racemic and enantioselective synthesis, reactivity, and biological properties associated with the xyloketal derivatives and their analogues.