Preparation and Suzuki-Miyaura coupling reactions of tetrahydropyridine-2-boronic acid pinacol esters

[reaction: see text] A study on the conversion of lactam-derived vinyl triflates and phosphates into the corresponding vinyl boronates was carried out. While delta-valerolactam-derived vinyl triflates were successfully converted into 1,4,5,6-tetrahydropyridine-2-boronic acid pinacol ester derivatives by Pd-catalyzed coupling reaction with both bis(pinacolato)diboron and pinacolborane, pyrrolidinone and epsilon-caprolactam derivatives either did not react or were readily reduced. The delta-valerolactam-derived vinyl boronates are thermally stable compounds that efficiently coupled, under Pd catalysis, with structurally diverse aryl and heteroaryl bromides and triflates, vinyl iodides and bromides, and aromatic acid chlorides, to give the corresponding 2-substituted piperidines in good to excellent yields. The number of electrophiles that can virtually be coupled with these new boronic esters makes them very useful reagents for the synthesis of N-heterocyclic compounds.     

Interaction potential between two 16O nuclei derived from the Skyrme interaction

The energy functional for the Skyrme density-dependent force is used to calculate the interaction potential between two ¹⁶O nuclei. A two-centre harmonic oscillator potential is employed to construct the density and kinetic energy density of the ground state of the combined system and of the separated nuclei. The antisymmetrization effects are investigated. The relative motion of the nuclei is taken approximately into account and the energy dependence of the potential derived from the Skyrme force is presented.     

Redox Imbalance and Mitochondrial Release of Apoptogenic Factors at the Forefront of the Antitumor Action of Mango Peel Extract

Today, an improved understanding of cancer cell response to cellular stress has become more necessary. Indeed, targeting the intracellular pro-oxidant/antioxidant balance triggering the tumor commitment to cell demise could represent an advantageous strategy to develop cancer-tailored therapies. In this scenario, the present study shows how the peel extract of mango—a tropical fruit rich in phytochemicals with nutraceutical properties—can affect the cell viability of three colon cancer cell lines (HT29, Caco-2 and HCT116), inducing an imbalance of cellular redox responses. By using hydro-alcoholic mango peel extract (MPE), we observed a consistent decline in thiol group content, which was accompanied by upregulation of MnSOD—a mitochondrial scavenger enzyme that modulates the cellular response against oxidative damage. Such an effect was the consequence of an early production of mitochondrial superoxide anions that appeared after just 30 min of exposure of colon cancer cells to MPE. The effect was accompanied by mitochondrial injury, consisting of the dissipation of mitochondrial membrane potential and a decrease in the level of proteins localized in the mitochondrial membrane—such as voltage-dependent anion-selective channel (VDAC1), mitofilin, and some members of Bcl-2 family proteins (Mcl-1, Bcl-2 and Bcl-X_L)—with the mitochondrial release of apoptogenic factors (cytochrome C and AIF). The analysis of the cytotoxic effects exerted by the different constituents of MPE (gallic acid, mangiferin, citric acid, quinic acid, pentagalloyl glucose, and methyl gallate) allowed us to identify those phytochemicals responsible for the observed anticancer effects, sustaining their future employment as chemopreventive or therapeutic agents.     

超声速化学反应流动中燃料预喷研究述评

研制基于超声速燃烧的高效吸气式推进装置(运行Mach数在3.5以上)需要寻求改善混合效率的有效机制, 这对于采用常规碳氢燃料(特别是可以增加密度的液体燃料)的装置尤为重要. 延长混合时间的一种途径是在飞行器燃料室的上游喷入部分燃料. 壁面喷射一直是超声速气动力学最具挑战性的课题, 这里包括使比冲损失最小、改善燃料-空气的混合、减少入口段/燃烧室的相互作用以及增进火焰稳定性等. 综述了超声速入口段或燃烧室的隔离器中液体燃料(个别情况下为气体燃料)喷射的研究进展. 在这些研究中, 燃料都是从后掠型细支架尾迹中的壁面处喷射出来的, 动压比很低($q_{\rm {jet}}/q_{\rm {air}}$=0.6$\sim$1.5). 它们涉及入口段和燃烧室的隔离器中单个支架/喷射器的几何结构及其组合方式、各种各样的喷射条件、不同的引射剂, 并且评估了这些因素对于燃料羽流喷散、比冲损失以及混合效率的影响. 述评引用了46篇参考文献.     

PRODUCTION OF PIGMENT NANOPARTICLES USING A WET STIRRED MILL WITH POLYMERIC MEDIA

Pigment nanoparticles with a size range of 10-100 nm were produced from large agglonmerates via a stirred media mill operating in the wet-batch mode and using polymeric media,The effects of several operating variables such as the surfactant concentration,polystyrene media loading.and media size on the pigment size distribution of the product were studied.The process dynamics was also investigated.Dynamic light scattering and electron microscopy were used as the characerization techniques.The polymeric grinding media are found to be effective for the production of pigment nanoparticles.The experimental results suggest the existence of an optimum media size and surfactant concentration,A population balance model of the process reveals a transition from first-order breakage kinetice for rela-large agglomerates split in a first-order kinetics,with a delay period,for the smaller particles.The model implies that large agglomerates split in a first-order fashion whereas the breakage of individual naoparticles may depend on induced fatigue of the particles.     

Classical trajectory calculations with time-dependent forces in heavy-ion collisions

The applicability of a phenomenological time-dependent nucleus-nucleus potential to deep inelastic collisions is studied. We present its general shape and make a particular choice of the diabatic and adiabatic parts. From trajectory calculations we find that the angle-energy correlation is well described when a time-dependent friction force is used. We also compare our results to some TDHF calculations.     

Editorial for Focus Issue on Enabling Science and Technology for High-Speed Optical Communications

<正>Fiber optics underpins the communications infrastructure for the information society today. Cables consisting of hair-like fibers speed data around the globe in the form of rapid pulses of light. Modern telecom     

Preparation and cycloaddition reactions of enantiopure 2-(N-acylamino)-1,3-dienes for the synthesis of octahydroquinoline derivatives

Stille, Suzuki-Miyaura, and Sonogashira cross-coupling reactions were carried out with a glutarimide-derived vinyl phosphate, bearing a chiral auxiliary on the N atom, to prepare enantiopure 2-(N-acylamino)-1,3-dienes as partners in Diels-Alder reactions. The cycloadditions were performed with various dienophiles under thermal conditions, with or without Lewis acids. With maleimides, the preferential formation of endo cycloadducts was observed, whereas with acrylamides the exo approach prevailed. Furthermore, in the latter case, 6-substitued octahydroquinolinones were obtained in accordance with the predicted regioselectivity. Since diastereopure compounds were in all cases obtained either by chromatography or by crystallization, and because of the easy access to a variety of boronic acids, to be used in the coupling step, this methodology is useful for the short synthesis of differently substituted, enantiopure octahydroquinolinones amenable to further transformation into decahydroquinolines possessing interesting biological activities.     

The modified electronic mass approach for the adiabatic corrections in H2

A theory of the modified (distance dependent) electronic mass effect for two-electron diatomic molecules is presented. The modified electronic mass correction is compared with the diagonal Born-Oppenheimer correction to the potential energy curves of H₂, suggesting that the adiabatic correction is almost exactly accounted for by this effect.