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Coumarin derivatives occur widely in nature and have been a part of both traditional and modern advancements in synthesis and application. To date, thousands of coumarin derivatives have been synthesized in labs or isolated from plant and marine life. These are essentially 2-pyrone core fused with a benzene ring and belong to the family of aromatic oxygen heterocycles. Coumarin in conjugation with various other heterocyclic systems has provided a robust framework in tuning the properties associated with the parent structure. The frequency of reports increased for these biheterocyclic systems from the mid of the twentieth century. Biheterocyclic coumarins also attracted many organic, and pharmaceutical chemists as these systems serve as useful synthetic intermediates in the synthesis of analogs of existing drugs. Its application in the design of effective organocatalysts and chemosensors further extended its versatility. Coumarin biheterocyclic core is utilized in the rational design and tuning complex molecular entities in molecular recognition, analytical and material chemistry. This review will highlight the advancements in the synthesis and applications of coumarin-linked nitrogen, oxygen, and sulfur heterocycles. It will also engage an account of forming five-, six-, and seven-membered heterocyclic rings linked to coumarin core. Critical physicochemical properties coupled with its application will make this review handy for synthetic chemists and drug discovery labs. A comprehensive spectrum of literature in this review will facilitate further development in biheterocycles with promising applications in the future.