antituberculosis; enzyme-inhibition; antioxidant; anti-inflammatory etc. After introducing the synthesis of 3-acetylcoumarin, the review proceeds with a comprehensive presentation of the synthesis of coumarin-chalcones under various conditions. Last, the reactions of prepared coumarin-chalcones through different mechanisms and the outcomes achieved through such reactions are discussed. It is envisaged that this review will prompt researchers to expand on the knowledge gained in this field the last twenty years.