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A highly regioselective and transition-metal free one-pot arylation of chromenones with arylboronic acids has been achieved employing KSO. The procedure consists of a sequence of some reactions including an arylation/decarboxylation cascade and proceeds well in aqueous media to afford biologically interesting flavones and 3-arylcoumarins. This method exhibited excellent selectivity and functional group tolerance under mild conditions. The reaction also showed perfect efficacy for the preparation of styryl coumarins.

Two series of novel coumarin derivatives, substituted at 3 and 7 positions with aminoalkoxy groups, are synthesized, characterized, and screened. The effect of amine substituents and the length of cross‐linker are investigated in acetyl‐ and butyrylcholinesterase (AChE and BuChE) inhibition. Target compounds show moderate to potent inhibitory activities against AChE and BuChE. 3‐(3,4‐Dichlorophenyl)‐7‐[4‐(diethylamino)butoxy]‐2H‐chromen‐2‐one (4y) is identified as the most potent compound against AChE (IC50=0.27 μm). Kinetic and molecular modeling studies affirmed that compound 4y works in a mixed‐type way and interacts simultaneously with the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. In addition, compound 4y blocks β‐amyloid (Aβ) self‐aggregation with a ratio of 44.11 % at 100 μm and significantly protects PC12 cells from H2O2‐damage in a dose‐dependent manner.

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A palladium-catalyzed decarboxylative domino reaction of imidazo[1,2-a]pyridines and coumarin-3-carboxylic acids has been developed, which provides access to dibenzoisochromenoimidazo[1,2-a]pyridin-6-ones possessing six fused rings.

A new metal‐free decarboxylative coupling reaction between coumarin‐3‐carboxylic acid derivatives, formaldehyde, and amines is developed. The use of water as the solvent without using any catalyst or additive, excellent functional group tolerance, and good yields are the beneficial features of this synthetic pathway. The cholinesterase inhibitory activity of some selected target compounds is also evaluated.