AbstractBeing an important constituent of naturally occurring lactones with diverse biological activities and as a pivotal intermediate in heterocycle synthesis, the isocoumarin motif has claimed vast interest in synthetic and medicinal research. The methodologies for the synthesis of isocoumarins involve particularly metal‐catalyzed reactions as well as various intramolecular and intermolecular cyclization reactions. The transition metal complexes of palladium, copper, rhodium, ruthenium, iridium, nickel, zinc and silver are frequently used for the construction of this scaffold. Electrophilic cyclization, oxyboration, and iodocyclization reactions are also known to afford isocoumarins. This review article attempts to highlight the recent advances in their synthesis along with general aspects such as natural occurrence, biological activities, etc. of this particular heterocyclic scaffold.magnified image