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Costanzo P.,University della Magna Graecia Viale Europa | Cariati L.,University della Magna Graecia Viale Europa | Desiderio D.,University of Molise | Sgammato R.,Parthenope University of Naples | And 6 more authors.
ACS Medicinal Chemistry Letters | Year: 2016

An ecofriendly synthetic pathway for the synthesis of donepezil precursors is described. Alternative energy sources were used for the total synthesis in order to improve yields, regioselectively, and rate of each synthetic step and to reduce the coproduction of waste at the same time. For all products, characterized by an improved structural rigidity respect to donepezil, the inhibitor activity on AChE, the selectivity vs BuChE, the side-activity on BACE-1, and the effect on SHSY-5Y neuroblastoma cells viability were tested. Two potential new lead compounds for a dual therapeutic strategy against Alzheimers disease were envisaged. © 2016 American Chemical Society. Source

Nardi M.,University of Calabria | Sindona G.,University of Calabria | Costanzo P.,University della Magna Graecia Viale Europa | Oliverio M.,University della Magna Graecia Viale Europa | Procopio A.,University della Magna Graecia Viale Europa
Tetrahedron | Year: 2015

An operationally simple and environmentally benign catalytic procedure has been developed to selectively reduce different α,β-unsaturated ketones. The corresponding allylic alcohols are obtained with high chemo- and diastereoselectivity using Er(OTf)3 and NaBH4 in 2-MeTHF. This protocol reduces the amount of catalyst and NaBH4 needed, compared to classical procedures and the stages of extraction/purification are carried out in aqueous solutions avoiding the use of toxic solvents. Taking into account that Er(OTf)3 can be considered even less toxic than table salt and the 'greenness' of 2-MeTHF as a solvent, the system Er(OTf)3/2-MeTHF can be proposed as a cheap, efficient, and environmentally sustainable reduction system for the synthesis of allylic alcohols. © 2014 Elsevier Ltd. Source

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