Jingyu He

Ultrasound-mediated synthesis of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates catalyzed by 1-carboxymethyl-3-methylimidazolium tetrafluoroborate under solvent free condition.

4-Substituted 1,4-dihydropyridine-3,5-dicarboxylates (4) have been synthesized by the solvent-free reaction of aldehyde, methyl propiolate and ammonium carbonate catalyzed by ionic liquid 1-carboxymethyl-3-methylimidazolium tetrafluoroborate under ultrasonic irradiation. The effects of changes in the ultrasonic power, temperature, catalysts and reactants on the synthesis of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates (4) are discussed. With the optimized reaction conditions, various aldehydes were used to synthesize 1,4-dihydropyridines (4) under the influence of ultrasound irradiation. Compared with the conventional thermal methods, the remarkable advantages of this method are the simple experimental procedure, shorter reaction time (2-10min) and high yield of product (76-95%). Furthermore, the green catalytic system can be recycled specific times without significantly decreasing the yields and reaction rates.

Crystal structure of (3aR,8aS,9aS)-8a-methyl-3,5-dimethylenedecahydronaphtho[ 2,3-b]furan-2(3H)-one, C15H20O2

Abstract C15H20O2, orthorhombic, P212121 (no. 19), a = 6.5445(5) Å, b = 8.7394(6) Å, c = 22.794(2) Å, V = 1303.7 Å3, Z = 4, Rgt(F) = 0.0748, wRref(F2) = 0.1419, T = 298 K.

A green method for synthesis of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives catalyzed by N-methylpyrrolidone hydrosulfate ([Hnmp]HSO4) ionic liquid

An efficient and green approach for the synthesis of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives is described via one-pot, three-component condensation of arylpyruvic acids, thiosemicarbazide, and 2-bromoacetophenones in the presence of N-methylpyrrolidone hydrosulfate ([Hnmp]HSO4) ionic liquid as the catalyst and solvent. This green catalyst can be recycled several times without any substantial decrease in the yields and reaction rates. The catalyst loadings are high.Graphical abstract

Design, Synthesis, and Evaluation of 7H-thiazolo-[3,2-b]-1,2,4-triazin-7-one Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimers disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of 7H‐thiazolo[3,2‐b]‐1,2,4‐triazin‐7‐one derivatives 6a–j were synthesized and investigated for their ability to inhibit the activity of human AChE (hAChE) in comparison with huperzine‐A. All the compounds were found to inhibit AChE activity, especially compounds 6c and 6i with the inhibition value of 76.10% and 77.82%, respectively. The molecular docking study indicated that they were nicely accommodated by AChE. The molecular docking study revealed that 6c and 6i possessed a more optimal binding conformation than 6a and can perfectly fit into the active and peripheral site of hAChE, and consequently exhibited highly improved inhibitor potency to hAChE.

Design, One-Pot Synthesis, and Evaluation of 7H-Thiazolo[3,2-b]-1,2,4-Triazin-7-One Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

In order to study the the structure-AChE inhibitory activity relationships of 7H-thiazolo [3,2-b]-1,2,4-triazin-7-one derivatives, the 7H-thiazolo[3,2-b]-1,2,4-triazin-7-ones were designed by molecular docking, and readily prepared via a one-pot reaction in N-methyl pyrrolidone hydrosulfate ([Hnmp]HSO4) lonic liquid. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control drug. Most of the target compounds exhibited more than 50% inhibition at 10μM.