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Tubulin binding agents and corresponding prodrug constructs

A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Extracurricular laboratory:new discovery of Bis(acetylacetone)copper

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ALLYLIC VERSUS VINILIC OXIDATION OF CYCLOHEXENE PROMOTED BY TRANSITION METAL beta-DIKETONATES

We report the cyclohexene oxidation by molecular oxygen in the presence of several metal beta-diketonates. The catalytic conditions used showed an allylic/vinilic oxidation (ao/av) ratio equal 1.5. The complexes M(l)n were used with the metal ions Co(III), Ni(II), Pd(II), Cu(II), chelated with acetylacetone (AcAc), benzoylacetone (BeAc) and dibenzoylacetone (BeBe) as ligands. The oxidation selectivity of the studied system suggests a different allylic/vinylic pathway compared with that observed inprevious reports.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Properties and Exciting Facts About 1317-39-1

HPLC of Formula: Cu2O, If you are hungry for even more, make sure to check my other article about HPLC of Formula: Cu2O

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N2O decomposition over CuO/CeO2catalyst: New insights into reaction mechanism and inhibiting action of H2O and NO by operando techniques

In this work, a combination of ex situ (STEM-EELS, STEM-EDX, H2-TPR and XPS), in situ (CO-DRIFTS) and operando (DR UV-vis and DRIFTS) approaches was used to probe the active sites and determine the mechanism of N2O decomposition over highly active 4 wt.% Cu/CeO2catalyst. In addition, reaction pathways of catalyst deactivation in the presence of NO and H2O were identified. The results of operando DR UV-vis spectroscopic tests suggest that [Cu-O-Cu]2+sites play a crucial role in catalytic N2O decomposition pathway. Due to exposure of {1 0 0} and {1 1 0} high-energy surface planes, nanorod-shaped CeO2support simultaneously exhibits enhancement of CuO/CeO2redox properties through the presence of Ce3+/Ce4+redox pair. Its dominant role of binuclear Cu+site regeneration through the recombination and desorption of molecular oxygen is accompanied by its minor active participation in direct N2O decomposition. NO and H2O have completely different inhibiting action on the N2O decomposition reaction. Water molecules strongly and dissociatively bind to oxygen vacancy sites of CeO2and block further oxygen transfer as well as regeneration of catalyst active sites. On the other hand, the effect of NO is expressed through competitive oxidation to NO2, which consumes labile oxygen from CeO2and decelerates [Cu+Cu+] active site regeneration.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Extracurricular laboratory:new discovery of Cuprous thiocyanate

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A single-helix copper-containing coordination polymer of dihydroglyoxaline sulfide formed in situ through oxidation of 1,3-imidazolidine-2-thione

A novel single-stranded helix coordination polymer [Cu(L)(SO4)(H2O)] (L = dihydroglyoxaline sulfide) was synthesized and characterized by single-crystal X-ray diffraction, IR, and TGA analysis. The polymer is an unprecedented 1D helical polymer based on a sulfate bridge and a dihydroglyoxaline sulfide chelating ligand. Both ligands were formed in situ through copper-mediated oxidation of 1,3-imidazolidine-2-thione. The helical chain is interlocked with each other through strong hydrogen bonding interactions to form a 2D sheet, which then stacks together to generate a 3D hydrogen bonding network.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Separation of propylene and propane by alkylimidazolium thiocyanate ionic liquids with Cu+ salt

Ionic liquids (ILs) coupled with Ag+ or Cu+ salts to form a new kind of reactive absorbent have been studied to separate light olefin from paraffin recently. In this work, we prepared two halogen-free alkylimidazolium thiocyanate ILs with cheaper cuprous thiocyanate, i.e., [Bmim]SCN-CuSCN and [Emim]SCN-CuSCN (Bmim, 1-butyl-3-methylimidazolium; Emim, 1-ethyl-3-methylimidazolium) and investigated their absorption capability for propylene, propane and mixture of both at 1-7 bar and 298-318 K. The effects of operating parameter including cation nature, temperature, pressure, Cu+ concentration and reuse of absorbent were investigated. Propylene shows a chemical absorption while propane does a physical one, and increasing Cu+ concentration effectively improves the absorption capability for propylene and the selectivity of propylene/propane. [Bmim]SCN-CuSCN has higher absorption capability and selectivity for propylene than [Emim]SCN-CuSCN, e.g., [Bmim]SCN-CuSCN-1.5 M can absorb 0.12 mol of propylene per liter while 0.012 mol of propane per liter at 1 bar and 298 K, with a selectivity of 10, which is comparable to some other ILs-Ag+ salts and better than pure ILs. Such absorbents can be regenerated through temperature and pressure swing without remarkable activity loss. This work shows that alkylimidazolium thiocyanate ILs with Cu+ salts are promising reactive absorbents to separate propylene from propane.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Final Thoughts on Chemistry for Bis(acetylacetone)copper

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Creation of RT-FM in CdO nanocrystalline powder by codoping with Cu and Gd: Effect of annealing in hydrogen atmosphere

Cadmium oxide codoped with Cu and Gd ions powders were synthesised by simultaneous thermal co-decomposition of a mixture of cadmium acetate dihydrate, bis(acetylacetonato)copper, and tris(acetylacetonato)gadolinium(III) complexes. The mass ratio of Cu/Cd is fixed while the Gd/Cd mass ratio varied systematically. The purpose of the present study is to prepare powders having room temperature ferromagnetic (RT-FM) properties. Thus, an amount from each powder was annealed in hydrogen atmosphere in order to study its influence on the magnetic properties. X-ray fluorescence (XRF) and X-ray diffraction (XRD) methods confirm the purity and the formation of single nanocrystalline structure of the as-prepared powders, thus, both Cu and Gd ions were incorporated into CdO lattice forming solid solutions. Magnetic measurements reveal that all doped CdO powders gained paramagnetic (PM) properties where the susceptibility increases linearly with increasing dopant Gd content; the measured effective magnetic moment of doped Gd3+ was 7muB. Furthermore, the created RT-FM is dependent on the Gd% doping level. Also, it was found that the hydrogenation of the powders slightly enhances their PM properties and strongly enhances or creates RT-FM. For hydrogenated CdO powder doped with 3.1% Gd, the coercivity (Hc), remanence (Mr), and saturation magnetization (Ms) were 283.2 Oe, 2.04 memu/g, and 6.67 memu/g, respectively. Also, under hydrogenation, the values of Hc, M r, and Ms were increased by ?145%, 476%, and 131%, respectively in comparison with as prepared. Thus it was proved, for the first time, the possibility of production of CdO with RT-FM, where magnetic characteristics can be tailored by doping and post treatment under H2 atmosphere, thus a new potential candidate to be used as a dilute magnetic semiconductor (DMS).

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Tetraheterosubstituted methanes with a carbon-halogen bond (update 2018)

In this chapter, recent methods for the preparation and elaboration of various substituted halomethanes are summarized. In addition to updates on classical methods, recently developed procedures employing new fluorinating agents, such as Togni’s reagents, are also presented. These methods are also put in the context of the synthesis of biologically active compounds.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Simple exploration of 1111-67-7

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Preparation of structurally modified, conductivity enhanced-p-CuSCN and its application in dye-sensitized solid-state solar cells

A method is found to significantly improve the p-type conductivity of CuSCN modified by incorporating triethylamine coordinated Cu(II) sites in its structure. It is done by mixing triethylamine hydrothiocyanate with CuSCN in propyl sulfide solution and allowing it to stand still in the dark for a few weeks in a closed sample tube. XRD and SEM analyses point to the modification of the CuSCN material. The Hall effect measurements clearly show a significant enhancement of hole concentration and hence of p-type conductivity. A maximum conductivity of 1.42 S m?1 is achieved for the structurally modified CuSCN compared to that of 0.01 S m?1 for ordinary CuSCN. AC impedance analysis of solid-state dye-sensitized solar cells based on this material clearly shows the reduction of bulk resistance of the cell with the use of modified CuSCN. This decrease in resistance has been attributed to the enhancement of conductivity and better pore filing of modified CuSCN inside the TiO2 matrix. As such, the solar cell performance gradually increases to an optimum value beyond which it decreases. The best result obtained for conversion efficiency is 3.4% at AM 1.5, which is a 41.8% enhancement from the best reported value for a dye-sensitized solid-state solar cell using CuSCN as a hole conducting material. The best efficiency value obtained is 14 times higher than that obtained for the dye-sensitized solid-state solar cell made with ordinary CuSCN.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

A new application about Bis(acetylacetone)copper

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Line-beam scan irradiation for preparation of YBCO films with high-Jc by excimer-laser-assisted MOD (ELAMOD)

Preparation of epitaxial YBa2Cu3O7 (YBCO) films on cerium oxide-buffered sapphire (r-cut alpha-Al2O3) substrates by an excimer-laser-assisted metalorganic deposition (ELAMOD) is reported. The ELAMOD process has been developed to bring about the advantage of shorter heating time than that in the conventional metalorganic deposition; the coated films are irradiated by an excimer laser beam before firing. We initiated the ELAMOD-YBCO process using a homogenized 8-mm-square laser beam which irradiates the coated surface in a fixed substrate mode. In order to extend the process applicable to large-area films, a scan irradiation mode was employed and a high critical-current density over 6 MA/cm2 has been observed. In the process, an appropriate choice of laser energy is difficult but crucial to obtain YBCO films with high superconducting properties. Then, laser irradiation from backside of the substrate was examined and proved to be beneficial to extend the experimental window of the laser energy. Moreover, a newly developed ELAMOD process using a 90-mm-wide line-beam is also reported which has a potential ability for large-area applications.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Final Thoughts on Chemistry for 1111-67-7

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Synthesis, characterization, crystal structures and photophysical properties of copper(I) complexes containing 1,1?-bis(diphenylphosphino) ferrocene (B-dppf) in doubly-bridged mode

Five copper(I) complexes having general formula [Cu2(mu-X) 2(kappa2-P,P-B-dppf)2] (X = Cl(1), Br(2), I(3), CN(4), and SCN(5)) were prepared starting with CuX and B-dppf in 1:1 molar ratio in DCM-MeOH (50:50 V/V) at room temperature. The complexes have been characterized by elemental analyses, IR, 1H NMR, 31P NMR and electronic spectral studies. Molecular structures for 1, 2 and 4 were determined crystallographically. Complexes 1, 2 and 4 exist as centrosymmetric dimers in which the two copper atoms are bonded to two bridging B-dppf ligands and two bridging (pseudo-)halide groups in a mu-eta1 bonding mode to generate nearly planar Cu2(mu-eta1-X)2 framework. Both bridging B-dppf ligands are arranged in antiperiplanar staggered conformation in 1 and 2 (mean value 56.40-56.76), and twisted from the eclipsed conformation (mean value 78.19) in 4. The Phi angle value in 4 is relatively larger as compared to 1 and 2. This seems to indicate that the molecular core [Cu2(mu-eta1-X)2] in 4 is a sterically demanding system that forces the B-dppf ligand to adopt a relatively strained conformation in comparison to less strained system in 1 and 2. All the complexes exhibit moderately strong luminescence properties in the solution state at ambient temperature.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”