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[From equivalent EP0480714A2] Compounds of the form, J-B-B-G-B-B-J wherein G is a dipeptide isostere, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.psi

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Despite many recent advances in the radical alkylation of electron-deficient heteroarenes since the seminal reports by Minisci and co-workers, methods for the direct incorporation of tertiary alkyl substituents into nitrogen heteroarenes are limited. This report describes the use of tert-alkyl oxalate salts, derived from tertiary alcohols, to introduce tertiary substituents into a variety of heterocyclic substrates. This reaction has reasonably broad scope, proceeds rapidly under mild conditions, and is initiated by either photochemical or thermal activation. Insights into the underlying mechanism of the higher yielding visible-light initiated process were obtained by flash photolysis studies, whereas computational studies provided insight into the reaction scope.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. Related Products of 108-47-4, In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. 108-47-4, name is 2,4-Dimethylpyridine. In an article,Which mentioned a new discovery about 108-47-4

We present a novel series of HIV integrase inhibitors, showing IC50s ranging from 0.01 to over 370 muM in an enzymatic assay. Furthermore, pharmacophore modeling study for the inhibitors was carried out to elucidate the structure-activity relationships. Finally, we found a 3D-pharmacophore model, which is composed of a hydrophilic and a hydrophobic domain, providing valuable information for designing other novel types of integrase inhibitors.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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The synthesis of pyridines from mixtures of aldehydes or ketones and NH3 in the liquid phase has been reinvestigated, using continuous dosage of the carbonyl components to the reaction mixture.The main product from the reaction of acetaldehyde and formaldehyde is 3-methylpyridine (6), which is also the main product from the reaction of acrolein or a mixture of crotonaldehyde and formaldehyde under the same conditions.The reaction of other aldehydes with formaldehyde give 3,5-dialkylpyridines, e.g. 10, 16.Acetone reacts with either formaldehyde or acetaldehyde to give polysubstituted alkylpyridines.A mechanistic pathway is proposed which accounts for the formation of the observed products.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Top Picks: new discover of 2,4-Dimethylpyridine

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Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media,Synthetic Route of 108-47-4, Name is 2,4-Dimethylpyridine, belongs to chiral-nitrogen-ligands compound, is a common compound. Synthetic Route of 108-47-4, In an article, authors is Vega, once mentioned the new application about Synthetic Route of 108-47-4.

Solvent degradation and volatile compound emissions are two of the major concerns about the deployment of carbon capture technologies based on chemical absorption. In this context, partial oxy-combustion might reduce the solvent degradation due to the use of a higher CO2 concentrated flue gas. This work evaluates the oxidative degradation of a novel AMP/AEP blend, namely POS #1, under partial oxy-combustion conditions. The effects of temperature and flue gas composition were evaluated in terms of solvent loss, degradation rates, NH3 emissions and degradation products. The experiments were set at temperatures up to 70 C and two levels of O2 concentration ? 3%v/v and 6%v/v. The CO2 concentration of the flue gas ranged between 15%v/v and 60%v/v CO2. The novel solvent POS#1 showed high resistance to degrade and resulted in lower degradation rates than MEA in all the operating conditions evaluated in this work. The maximum degradation of AEP and AMP was 24% and 19%, respectively. MEA degraded almost double under the same conditions. Temperature and O2 concentration enhanced the oxidative degradation of POS #1. However, the use of higher CO2 concentration in the flue gas led to lower degradation rates of AEP and AMP and hence oxidative degradation was partially inhibited under partial oxy-combustion conditions. The presence of higher CO2 content in the flue gas decreased the NH3 production and a 70% reduction of its emissions was achieved as the CO2 concentration shifted from 15%v/v to 60%v/v. Other major degradation compounds such as formate and 2,4-lutidine were also decreased. New degradation products were not identified so that the suggested degradation pathways proposed in the literature were not influenced by the presence of higher CO2 concentrations.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Application of 108-47-4, Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. 108-47-4, Name is 2,4-Dimethylpyridine,belongs to chiral-nitrogen-ligands compounds, now introducing its new discovery.

Three adducts of zinc azide with 2,4-/3,4- and 3,5-dimethylpyridine (DMP), respectively, were prepared and the crystal structures determined by single crystal X-ray diffraction methods.The three compounds crystallize in the monoclinic space group P21/c with Z = 4: Zn(N3)2*2,4-DMP at 300(2) K: a = 1098.6(4), b = 1600.2(6), c = 608.8(3) pm, beta = 102.47(3) deg; R = 0.071 (RW = 0.056).Zn(N3)2*3,4-DMP at 103(3) K: a = 1102.1(3), b = 1.649.0(4), c = 611.8(1) pm, beta = 104.54(2) deg; R = 0.055 (RW = 0.051).Zn(N3)2*3,5-DMP at 97(3) K: a = 602.1(2), b = 2037.9(7), c = 853.8(3) pm, beta = 90.77(3) deg; R = 0.069 (RW = 0.055).The molecular geometry is similar for the three adducts, but the packing of the DMP-molecules is different.The zinc atoms are surrounded by five nitrogen atoms, four belonging to the azide groups and one to the DMP-adduct.The trigonal bipyramidal shaped ZnN5-polyhedra share common edges to form chains.Keywords.Azide; Crystal structure; Dimethylpyridine; Zinc.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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The use of phosphogypsum, which is a waste product of the phosphorus fertilizer industry, as a heterogeneous catalyst in condensation of acetylacetone, acetylene, and ammonia is considered.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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The 13C NMR spectra of 22 alkyl-substituted 9aH-quinolizine-1,2,3,4-tetracarboxylates have been obtained and X-ray analyses have been performed for three of them.The chemical shift differences between the parent 9aH-quinolizine and the methyl-substituted compounds can only be interpreted in terms of the usual alpha and beta effects for 8-methyl-9aH-quinolizine. 6-, 7-, 9-, and 9a-methyl substituents cause not only a very large deshielding of the carbon at the position of substitution together with shielding changes at adjacent atoms, but also influence the shieldings of the other carbons in both rings of the compounds under study.The observed changes are interpreted in terms of steric hindrance between the methyl groups of ring B and the ester groups of ring A, and hyperconjugative effects introduced by the methyl groups.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of beta-adrenergic signaling in vitro studies. Hydrazone derivative 5 and 1,2,4-triazole derivative 24a were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity toward GRK2 and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, and 7 with almost equipotent inhibition to GRK3. Our medicinal chemistry efforts led to the discovery of 115h (GRK2 IC50 = 18 nM), which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates beta-adrenergic receptor (betaAR)-mediated cAMP accumulation and prevents internalization of betaARs in beta2AR-expressing HEK293 cells treated with isoproterenol. Therefore, 115h appears to be a novel class of therapeutic for heart failure treatment.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Related Products of 126456-43-7, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 126456-43-7, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol,introducing its new discovery.

A small library of ninety four uridine antibiotic analogs was synthesized, under the Pilot Scale Library (PSL) Program of the NIH Roadmap initiative, from amine 2 and carboxylic acids 33 and 77 in solution-phase fashion. Diverse aldehyde, sulfonyl chloride, and carboxylic acid reactant sets were condensed to 2, leading after acid-mediated hydrolysis, to the targeted compounds 3-32 in good yields and high purity. Similarly, treatment of 33 with diverse amines and sulfonamides gave 34-75. The coupling of the amino terminus of d-phenylalanine methyl ester to the free 5?-carboxylic acid moiety of 33 followed by sodium hydroxide treatment led to carboxylic acid analog 77. Hydrolysis of this material gave analog 78. The intermediate 77 served as the precursor for the preparation of novel dipeptidyl uridine analogs 79-99 through peptide coupling reactions to diverse amine reactants. None of the described compounds show significant anticancer or antimalarial acivity. A number of samples exhibited a variety of promising inhibitory, agonist, antagonist, or activator properties with enzymes and receptors in primary screens supplied and reported through the NIH MLPCN program.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis