The coumarin scaffold is an important structure in medicinal chemistry because it is found in several naturally occurring molecules which exhibit a variety of biological activities, such as anti-cancer, anti-inflammatory, anti-diabetic, antimicrobial, and antiviral, antifungal. In addition, various synthetic coumarins motifs are present in marketed drugs. They are also involved in the actions of the photosynthesis, control of respiration, plant growth hormones and growth regulators, and also defense against infection. This review will provide an overview of coumarin moieties with medicinal aspects synthesized in the last 15 years and will cover the most potent molecule in each report. In this review, different synthesis methods of coumarin and their derivatives have been covered.