Synthesis of Acyclic Nucleosides with N‐[(Benzyloxy)(aryl)methyl] Substituents as Potential HEPT,EBPU, and TNK‐651 Analogues

The syntheses of the novel acyclic nucleosides 5a – 5m , carrying different N‐[(benzyloxy)(aryl)methyl] substituents, are described (Scheme). These compounds could be prepared in medium‐to‐good yields by either direct or silyl‐assisted coupling of the electrophiles 6 with either purine or pyrimidine nucleobases, or with different imidazole derivatives. The reactivity of the positively charged electrophilic intermediates derived from 6 upon Cl^? abstraction was rationalized by ab initio HF/6‐311G quantum‐mechanic calculations. The positive charge was found to be dispersed differently, depending on the electronic properties of the aryl substituents.     

Thermal and morphological characteristics of solution blended epoxy/NBR compound

Systematic study about the effect of acrylonitrile–butadiene rubber (NBR) concentration on the fracture toughness and thermal behavior of epoxy resin is conducted in this study. NBR is solved in an aromatic hydrocarbon solvent and is added to epoxy resin. We used diethylene-teriamin as the curing agent for epoxy resin. Tensile test results, performed followed by molding procedure, show that the toughness is improved owing to the increase of rubber content. Scanning electron microscopy (SEM) and atomic force microscopy besides thermogravimetric analysis (TG) are used to investigate the epoxy/rubber interface and chemical decomposition of the resultant mixture. The thermal behavior of cured epoxy resin was analyzed via TG instrument at different heating rates. Thermogravimetry curves showed that the thermal decomposition of epoxy system was occurred in only one stage regardless of the rubber content. The apparent activation energies of the rubber/epoxy systems containing 0, 5, and 10 phr of rubber were determined by Flynn–Wall–Ozawa, Kissinger–Akahira–Sunose, and Friedman methods. The results prove that the thermal stability of epoxy resin was decreased with enhancing the rubber content. However, the trend of changing activation energy versus conversions is totally different followed by adding the elastomer to the system compared to neat epoxy resin. Moreover, the results obtained via our proposed facile solution blending method are compared to those of resins modified with nano-powdered elastomer.     

Simultaneous determination of adrenaline,uric acid,and cysteine using bifunctional electrocatalyst of ruthenium oxide nanoparticles

In this study, ruthenium oxide nanoparticles were electrochemically deposited on the surface of a glassy carbon electrode (RuON-GCE). Electrochemical studies indicate that a modified electrode (RuON-GCE) plays the role of an excellent bifunctional electrocatalyst for the oxidation of adrenaline (AD) and uric acid (UA) in two different potentials. The charge transfer coefficient (α) and the heterogeneous charge transfer rate constant (k′) between the analytes and the electrodeposited nanoparticles were determined using cyclic voltammetry experiments. Through a different pulse voltammetric (DPV) method, the plot of the electrocatalytic current versus AD and UA concentrations emerged to be constituted of two linear segments with different sensitivities. Furthermore, the detection limits of AD and UA were estimated. In DPV, RuON-GCE could separate the oxidation peak potentials of AD, UA, and cysteine (Cys) present in the same solution though, at the bare GCE, the peak potentials were indistinguishable. Finally, the modified electrode activity was studied for the electrocatalytic determination of AD in an injection solution and UA in a human urine sample. The results were found satisfactory.     

One-pot synthesis of N-alkyl purine and pyrimidine derivatives from alcohols using TsIm: a rapid entry into carboacyclic nucleoside synthesis

A convenient and efficient one-pot N-alkylation of nucleobases from alcohols using N-(p-toluenesulfonyl)imidazole (TsIm) is described. In this method, treatment of alcohols with a mixture of purine or pyrimidine nucleobase, TsIm, K₂CO₃, and triethylamine in refluxing DMF regioselectively furnishes the corresponding N-alkyl nucleobases in good yields. This methodology is highly efficient for various structurally diverse primary alcohols.     

Back propagation modeling of shear stress and viscosity of aqueous Ionic-MXene nanofluids

Journal of Thermal Analysis and Calorimetry - Back-propagation modeling of viscosity and shear stress of Ionic-MXene nanofluid is carried out in this work. The data for Ionic-MXene nanofluid of...     

An enantioselective chiral Brønsted acid catalyzed imino-azaenamine reaction

The enantioselective Br?nsted acid catalyzed addition of methyleneaminopyrrolidine to N-Boc imines has been achieved in the presence of chiral phosphoric acids derived from 3,3'-di(phenanthryl)-H8-BINOL. The corresponding aminohydrazones have been isolated in good yields with enantiomeric excesses up to 90%. [reaction: see text]     

Makespan minimization for parallel machines scheduling with multiple availability constraints

The problem of makespan minimization for parallel machines scheduling with multiple planned nonavailability periods in the case of resumable jobs is considered. In the current state of the literature, there is a limited number of models and algorithms dealing with this problem and only for very small problem size, and nonavailability limited to some machines. The problem is first formulated as a mixed integer linear programming model and optimally solved using CPLEX for small to moderately large size problems with multiple availability constraints on all machines. An implicit enumeration algorithm using the lexicographic order is then designed to solve large-scale problems. Numerical results are obtained for several experiments and they show the validity and performance improvements procured by both the MILP model and the new enumeration algorithm.     

\hbox {Ph}_{3}\hbox {P/CCl}_{4} as a highly efficient reagent for one-pot N-alkylation of sulfonamides from alcohols: a rapid route to N-alkyl sulfonamides synthesis

A mild, efficient, and selective protocol for the one-pot $N$ -alkylation of sulfonamides with alcohols using triphenylphosphine and carbon tetrachloride is described. In this method, treatment of alcohols with a mixture of triphenylphosphine, carbon tetrachloride, and potassium sulfonylamide salts in refluxing anhydrous DMF furnishes the corresponding $N$ -alkyl sulfonamides in good to excellent yields. This protocol is highly efficient for various structurally diverse alcohols and potassium sulfonylamide salts. In this paper the influence of solvents and various reagents as sources for electrophilic-halogen instead of carbon tetrachloride in combination with triphenylphosphine have been examined. This protocol demonstrates the selectivity between primary and secondary alcohols. A plausible mechanism for this protocol has been described.     

A novel primary amine-based anion exchange membrane adsorber

A novel anion exchange membrane adsorber is presented which shows excellent impurity removal under different buffer conductivities ranging from 2 to 2 7mS/cm. The membrane utilizes a primary amine ligand (polyallylamine) and was designed specifically to bind impurities at high salt concentrations. Studies with DNA, endotoxin, and virus spiked into buffer at varying salt conditions were done, resulting in clearance of >3, 4, and 4 LRV, respectively, with negligible change on increasing salt up to 27 mS/cm conductivities. Verification of virus removal in mAb feedstocks is also shown. The data are compared with other membrane adsorbers and a conventional resin which utilize traditional chemistries to demonstrate improved purification performance with the primary amine ligand. Additional data on scale-up of the membrane adsorber device is discussed. A stacked flat-sheet design was implemented to ensure linear scale-up of performance using bovine serum albumin (BSA) as a model. The linearly scalable device, coupled with the highly effective membrane for virus, DNA, and endotoxin removal, represents a step forward in polishing technology for the purification of monoclonal antibodies and recombinant proteins.     

Should the AOAC use-dilution method be continued for regulatory purposes?

Despite its very poor reproducibility, AOAC INTERNATIONAL's use-dilution method (UDM) for bactericidal activity (AOAC Methods 964.02, 955.14, and 955.15) has been required by the U.S. Environmental Protection Agency (EPA) since 1953 for regulatory purposes, while methods with better reproducibility have been adopted in Canada and Australia. This study reviews UDM from a statistical perspective. Additionally, the test's expected results were compared to those obtained from actual evaluation of several formulations. Significant gaps have been identified in the reproducibility of the test data as predicted by statistical analysis and those presented to the EPA for product registration. UDM's poor reproducibility, along with its qualitative nature, requires the concentration of the active ingredient to be high enough to ensure all or most carriers to be free of any viable organisms. This is not in accord with the current trends towards sustainability, human safety, and environmental protection. It is recommended that the use of the method for regulatory purposes be phased out as soon as possible, and methods with better design and reproducibility be adopted instead.