RT Journal Article
T1 Straightforward Synthesis of Bis[(trifluoromethyl)sulfonyl]ethylated Isocoumarins from 2-Ethynylbenzoates
A1 Petcu, Sonia
A1 Lázaro Milla, Carlos
A1 Rodríguez, Javier
A1 Iriepa, Isabel
A1 Bautista-Aguilera, Óscar
A1 Aragoncillo Abanades, Cristina
A1 Alonso Gómez, José Miguel
A1 Almendros Requena, Pedro
AB 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.
PB American Chemical Society
SN 0022-3263
YR 2023
FD 2023
LK https://hdl.handle.net/20.500.14352/91922
UL https://hdl.handle.net/20.500.14352/91922
LA eng
NO Petcu A S, Lázaro-Milla C, Rodríguez F J, Iriepa I, Bautista-Aguilera, Ó M, Aragoncillo C, Alonso J M, Almendros P. Straightforward Synthesis of Bis[(trifluoromethyl)sulfonyl]ethylated Isocoumarins from 2-Ethynylbenzoates. J. Org. Chem. 2023 , 88, 7373-7380.
NO Ministerio de Ciencia e Innovación (España)
NO Consejo Superior de Investigaciones Cieníficas 
NO European Commission
DS Docta Complutense
RD 6 oct 2024