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Coumarins are privileged structures owing to their well-established biological and physicochemical properties. There are several methods for the synthesis of coumarins, among them the Pechmann reaction using phenols and ehyl acetoacetate, which leads to the formation of 4-methylcoumarins in good yields. Using Huisgen Reaction, the incorporation of monosubstituted 1,2,3-triazole units through copper-catalyzed azide–alkyne cycloaddition (CuAAC) reactions provides a straightforward approach to the preparation of hybrid molecular libraries. Continuing our studies of antitumor activity, in this work we explore these two reactions for the synthesis of a novel chemical library of coumarin/1,2,3-triazole hybrids. The methodology described herein demonstrated broad synthetic applicability under mild conditions, employing green solvent systems without external heating. The resulting functionalized derivatives explore a still underinvestigated position within the coumarin framework, this approach expands the chemical space of coumarin derivatives and offers a synthetic platform for the design of new biologically active molecules.
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