%0 Journal Article
%A Petcu, Sonia
%A Lázaro Milla, Carlos
%A Rodríguez,  Javier
%A Iriepa, Isabel
%A Bautista-Aguilera, Óscar 
%A Aragoncillo Abanades, Cristina
%A Alonso Gómez, José Miguel
%A Almendros Requena, Pedro
%T Straightforward Synthesis of Bis[(trifluoromethyl)sulfonyl]ethylated Isocoumarins from 2-Ethynylbenzoates
%D 2023
%@ 0022-3263
%U https://hdl.handle.net/20.500.14352/91922
%X Herein, we report a facile isocoumarin and isoquinolone preparation by taking advantage of an initial bis(triflyl)ethylation [triflyl = (trifluoromethyl)sulfonyl] reaction, followed by heterocyclization, which contrasts with our previous results on cyclobutene formation. The efficiency of the catalyst- and irradiation-free heterocyclization/bis(triflyl)ethylation sequence showed exquisite dependence on the electronic nature of the substituents at the 2-ethynylbenzoate(benzamide) precursors.Molecular docking of model bis(triflyl)ethylated isocoumarins on human acetylcholinesterase (hAChE) revealed promising biological activities through selective coordination on both the catalytic active site and peripheral active site.
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