The important role of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II)

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Synthesis of 3-alkyl enol mimics inhibitors of type II dehydroquinase: Factors influencing their inhibition potency

Several 3-alkylaryl mimics of the enol intermediate in the reaction catalyzed by type II dehydroquinase were synthesized to investigate the effect on the inhibition potency of replacing the oxygen atom in the side chain by a carbon atom. The length and the rigidity of the spacer was also studied. The inhibitory properties of the reported compounds against type II dehydroquinase from Mycobacterium tuberculosis and Helicobacter pylori are also reported. The binding modes of these analogs in the active site of both enzymes were studied by molecular docking using GOLD 5.0 and dynamic simulations studies.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Some scientific research about Bis(tri-tert-butylphosphine)palladium

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An atom efficient synthesis of tamoxifen

The direct carbolithiation of diphenylacetylenes and their cross-coupling procedure taking advantage of the intermediate alkenyllithium reagents are presented. By employing our recently discovered highly active palladium nanoparticle based catalyst, we were able to couple an alkenyllithium reagent with a high (Z/E) selectivity (10:1) and good yield to give the breast cancer drug tamoxifen in just 2 steps from commercially available starting materials and with excellent atom economy and reaction mass efficiency.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Simple exploration of 1,1′-Bis(di-tert-butylphosphino)ferrocene-palladium dichloride

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PROCESS FOR THE PREPARATION OF AROMATIC DERIVATIVES OF 1-ADAMANTANE

Process for the obtaining of 1 -adamantane (tricycle[3.3.1.1 (3,7)]decane) derivatives, or of a pharmaceutically acceptable salt thereof, based on a carboxylation reaction, via metallation, of a precursor compound with an adequate leaving group. It also comprises the preparation of the precursor compound by means of a selective coupling of the corresponding boron, magnesium or zinc derivative with the corresponding disubstitute aromatic derivative. It is especially useful for the obtaining of Adapalene at industrial scale with good yield and high purity.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Extended knowledge of 40691-33-6

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Chemistry informer libraries: A chemoinformatics enabled approach to evaluate and advance synthetic methods

Major new advances in synthetic chemistry methods are typically reported using simple, non-standardized reaction substrates, and reaction failures are rarely documented. This makes the evaluation and choice of a synthetic method difficult. We report a standardized complex molecule diagnostic approach using collections of relevant drug-like molecules which we call chemistry informer libraries. With this approach, all chemistry results, successes and failures, can be documented to compare and evolve synthetic methods. To aid in the visualization of chemistry results in drug-like physicochemical space we have used an informatics methodology termed principal component analysis. We have validated this method using palladium- and copper-catalyzed reactions, including Suzuki-Miyaura, cyanation and Buchwald-Hartwig amination.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

The Absolute Best Science Experiment for 52409-22-0

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Enhancing the photovoltaic properties of low bandgap terpolymers based on benzodithiophene and phenanthrophenazine by introducing different second acceptor units

Two novel donor-acceptor (D-A) type random conjugated terpolymers PBDTT-PPzIID and PBDTT-PPzDPP were synthesized by copolymerizing electron-rich alkylthienyl benzodithiophene (BDTT) and two different electron-deficient units, in which phenanthrophenazine (PPz) was the first acceptor unit, and isoindigo (IID) or diketopyrrolopyrrole (DPP) with a strong electron-withdrawing ability was the second acceptor unit, respectively. Compared to their parent polymer PTTPPz-BDTT, a broadening of the band in the long wavelength region from 500 to 850 nm and a significant decrease in HOMO levels were observed for the random terpolymers. Ca and PFN-Br were used as interfacial layers to optimize the devices, respectively. Pleasingly, after replacing Ca/Al with PFN-Br/Al as the cathode, the performance of both polymer devices improved greatly. A maximum power conversion efficiency (PCE) of 5.91% was obtained with a Voc of 0.73 V, a Jsc of 11.75 mA cm-2 and a FF of 68.8% in the PBDTT-PPzDPP/PC71BM-based device, while the PBDTT-PPzIID/PC71BM-based device achieved a PCE of 4.21%. To the best of our knowledge, this is one of the highest recorded FF values among PSCs based on previously reported phenazine copolymers.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Final Thoughts on Chemistry for 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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Compositions and methods for inducing cell dedifferentiation

The present invention provides compositions and methods for dedifferentiating lineage committed mammalian cells.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Brief introduction of 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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Synthetic Route of 95464-05-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.95464-05-4, Name is 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex, molecular formula is C35H32Cl4FeP2Pd. In a Patent£¬once mentioned of 95464-05-4

1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors

Compounds represented by Formula (I): 1or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Direct functionalization of the cyclometalated 2-(2?-pyridyl)phenyl ligand bound to iridium(III)

Treatment of [Ir(ppy)2(mu-Cl)]2 and [Ir(ppy) 2(dtbpy)][OTf] (ppy = 2-(2?-pyridyl)phenyl; dtbpy = 4,4?-di-tert-butyl-2,2?-bipyridine; OTf = triflate) with pyridinium tribromide in the presence of Fe powder led to isolation of [Ir(4-Br-ppy)(mu- Br)]2 (1) and [Ir(4-Br-ppy)2(dtbpy)][OTf] (2), respectively. Pd-catalyzed cross-coupling of 2 with RB(OH)2 afforded [Ir(4-R-ppy)2(dtbpy)][OTf] (R = 4?-FC6H4 (3)), 4?-PhC6H4 (4), 2?-thienyl (5), 4?-C6H4CH2OH (6). Treatment of 4 with B2(pin)2 (pin = pinacolate) afforded [Ir{4-(pin)B-ppy} 2(dtbpy)][OTf] (7). The alkynyl complexes [Ir(4-PhCC-ppy) 2(dtbpy)][OTf] (8) and [Ir{4-Me2(OH)CC-ppy}(4-Br-ppy) (dtbpy)][OTf] (9) were prepared by cross-coupling of 2 with PhCCSnMe3 and Me2C(OH)CCH, respectively. Ethynylation of [Ir(fppy) 2(dtbpy)][OTf] (fppy = 5-formyl-2-(2?-pyridyl)phenyl) with Ohira’s reagent MeCOC(N2)P(O)(OEt)2 afforded [Ir{5-HCC-ppy}2(dtbpy)][OTf] (10). The solid-state structures of 2, 5, 7, and 10 have been determined.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Discovery of a novel B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor by utilizing structure-based drug design

B-cell lymphoma 6 (BCL6) is a transcriptional repressor that can form complexes with corepressors via protein-protein interactions (PPIs). The complexes of BCL6 and corepressors play an important role in the formation of germinal centers (GCs), and differentiation and proliferation of lymphocytes. Therefore, BCL6-corepressor interaction inhibitors would be drug candidates for managing autoimmune diseases and cancer. Starting from high-throughput screening hits 1a and 2a, we identified a novel BCL6-corepressor interaction inhibitor 8c (cell-free enzyme-linked immunosorbent assay [ELISA] IC50=0.10muM, cell-based mammalian two-hybrid [M2H] assay IC50=0.72muM) by utilizing structure-based drug design (SBDD) based on an X-ray crystal structure of 1a bound to BCL6. Compound 8c also showed a good pharmacokinetic profile, which was acceptable for both in vitro and in vivo studies.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms

We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a “flat” GT1 mutant profile. This NS5A inhibitor contains a unique tetracyclic indole core while maintaining the imidazole-proline-valine Moc motifs of our previous NS5A inhibitors. Compound 40 is currently in early clinical trials and is under evaluation as part of an all-oral DAA regimen for the treatment of chronic HCV infection.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method