Abstract
Click chemistry has emerged as a valuable synthetic tool for the assembly of diverse molecular units. In particular, the copper-catalyzed azide–alkyne cycloadditions (CuAAC) revealed to be extremely versatile and are currently used for the synthesis of molecules with a wide range of applications. Accordingly, CuAAC reactions have been extensively used for the functionalization of phenolic compounds, many of them with well-known biological properties. Herein, an overview of the most important advances in the application of CuAAC reactions to chalcones and chromones, including flavones, since 2002 is presented. In particular, this review discusses the use of azidochalcones, azidochromones, alkynylchalcones and alkynylchromones in 1,3-dipolar cycloadditions. The biological properties of some of the resulting conjugates, where the two units are linked by a 1,2,3-triazole bridge, are also presented. In some reported examples, the new conjugates revealed additive activities which represent a promising step forward in medicinal chemistry.
Keywords: Chalcone, chromone, flavone, isoflavone, triazole, 1, 3-dipolar cycloaddition, click chemistry.
Graphical Abstract
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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