Facile synthesis of 4″-O-alkyl-(–)-EGCG derivatives through regioselective deacetylative alkylation

Therapeutic potential of the D-ring methyl ethers of (–)-epigallocatechin-3-gallate [(–)-EGCG] warrants extensive structure–activity relationship study of various D-ring ethers of (–)-EGCG but, for this purpose, efficient synthetic strategy needs to be developed. In this study, efficient preparation of the 4″-O-alkyl-(–)-EGCGs (4a–e) was demonstrated using KI/K₂CO₃-promoted deacetylative alkylation of peracetyl (–)-EGCG, which could be broadly utilized for the preparation of various D-ring alkyl ethers of (–)-EGCG and thereby extensive structure–activity relationship study.     

Direct Synthesis of Hydrogen Peroxide from Hydrogen and Oxygen Using Tailored Pd Nanocatalysts: A Review of Recent Findings

Direct synthesis of hydrogen peroxide from hydrogen and oxygen is being actively studied as an alternative to the current manufacturing process. The direct synthesis route has not reached the point of commercialization because of low yields, but significant effort is being spent on enhancing the productivity. With advances in computational capacity, simulation studies based on DFT calculations now offer directions for catalyst improvement, but such modifications can only be realized through the application of nanoparticle synthesis techniques that allow for nanocrystal morphology and size control and unique immobilization. To date, there have only been a small number of studies on such nanoparticles with size and crystallographic homogeneity for the direct hydrogen peroxide synthesis. According to our knowledge no other group has systematically investigated application of nanoparticles in direct synthesis of hydrogen peroxide, and thus included in this review are primarily previous studies conducted by our group. In this review, we discuss the utilization of nanotechnology for the synthesis of Pd catalysts and its effect on the direct synthesis of hydrogen peroxide, and we suggest a direction for future studies.     

Effect of Thermal Treatment on Preshaped Ionic Polymer Metal Composite (IPMC) Actuators

A new method to fabricate ionic polymer metal composite (IPMC) actuators with a 3-dimensional preshaped form by a simple thermal treatment process is demonstrated. The effects of the thermal treatment process on the properties of the actuator are analyzed and the characteristics of the actuator, such as stiffness, displacement and resonance, generating force, and repeated motions, are compared with those of unheated IPMC actuators. The experimental results show that thermal-treated IPMC actuators have improved generating force as well as preshaping of the 3-dimensional form.     

Determination of PF‐04620110, a novel inhibitor of diacylglycerol acyltransferase‐1, in rat plasma using liquid chromatography–tandem mass spectrometry and its application in pharmacokinetic studies

In this study, we developed a method for the determination of PF‐04620110 (2‐{(1r,4r)‐4‐[4‐(4‐amino‐5‐oxo‐7,8‐dihydropyrimido[5,4‐f][1,4]oxazepin‐6(5H)‐yl)phenyl]cyclohexyl}acetic acid), a novel diacylglycerol acyltransferase 1 (DGAT‐1) inhibitor, in rat plasma and validated it using liquid chromatography–tandem mass spectrometry (LC‐MS/MS). Rat plasma samples were processed following a protein precipitation method by using acetonitrile and were then injected into an LC‐MS/MS system for quantification. PF‐04620110 and imipramine (internal standard) were separated using a Hypersil Gold C₁₈ column, with a mixture of acetonitrile and 10 mm ammonium formate (90:10, v/v) as the mobile phase. The ion transitions monitored in positive‐ion mode [M + H]⁺ of multiple‐reaction monitoring were m/z 397.0 → 260.2 for PF‐04620110 and m/z 280.8 → 86.0 for imipramine. The detector response was specific and linear for PF‐04620110 at concentrations within the range 0.05–50 µg/mL and the signal‐to‐noise ratios for the samples were ≥10. The intra‐ and inter‐day precision and accuracy of the method matched the acceptance criteria for assay validation. PF‐04620110 was stable under various processing and/or handling conditions. PF‐04620110 concentrations in the rat plasma samples could be measured up to 24 h after intravenous or oral administration of PF‐04620110, suggesting that the assay is useful for pharmacokinetic studies in rats. Copyright © 2013 John Wiley & Sons, Ltd.     

Particle and breath figure formation of triblock copolymers having self‐complementary hydrogen‐bonding units

Novel triblock copolymers having self‐complementary hydrogen‐bonding units were synthesized by using reversible addition–fragmentation transfer polymerization. As characterized by dynamic light scattering and atomic force microscopy, these polymers formed noncovalently crosslinked polymer particles and showed an aggregation behavior by intermolecular and intramolecular interactions. At low concentration, polymers formed nanoparticles, and the particle diameter increased with increasing polymer concentration. Well‐ordered hexagonal microstructures were prepared by “Breath Figure” technique with the triblock copolymers. © 2012 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012