Dibutylamine-catalysed efficient one-pot synthesis of biologically potent pyrans
An expedient, eco-friendly and efficient procedure for the preparation of novel pyran derivatives has been developed through a solvent-free, one-pot reaction of various aldehydes, malononitrile and either methylacetoacetate or ethyl benzoylacetate in the presence of dibutylamine (2.5 mol %) at room temperature. This procedure is advantageous because it is mild, environmentally friendly, gives high yields and requires short reaction times. Furthermore, the product did not necessitate separation via extraction and column chromatography.
Synthesis of pyridinium-based salts: Catalytic application at the synthesis of six membered O-heterocycles
In this paper, a range of pyridinium-based ionic liquid (IL) and molten salts (MSs) with various counter ions were designed, synthesized and fully characterized. These novel ionic liquid and molten salts were prepared via the reaction of [PySO3
Babaee, Saeed,Zolfigol, Mohammad Ali,Zarei, Mahmoud,Abbasi, Maryam,Najafi, Zahra
(2019/06/27)
New tacrine-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates
A series of poly-functionalized tacrine-derived compounds namely 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates were designed and synthesized as cholinesterases inhibitors. The in?vitro inhibition assay against AChE and BuChE demonstrated that most of compounds had potent AChE inhibitory with reserving potential of BuChE inhibition. Among them, compound 6i bearing a 4-(3-bromophenyl) moiety showed the most potent activity against AChE/BuChE (IC50s values of 0.069 and 1.35?μM, respectively). The anti-AChE activity of 6i was five times more than that of tacrine. The SAR study revealed that chloro/bromo substituent at ortho or meta position of the 4-phenyl ring can improve the anticholinesterase activity.