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The glycolytic pathway has been considered a potential drug target against the parasitic protozoan species of Trypanosoma and Leishmania. We report the design and the synthesis of inhibitors targeted against Trypanosoma brucei phosphofructokinase (PFK) and Leishmania mexicana pyruvate kinase (PyK). Stepwise library synthesis and inhibitor design from a rational starting point identified furanose sugar amino amides as a novel class of inhibitors for both enzymes with IC50 values of 23 muM and 26 muM against PFK and PyK, respectively. Trypanocidal activity also showed potency in the low micromolar range and confirms these inhibitors as promising candidates for the development towards the design of anti-trypanosomal drugs.

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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 series of new chiral 6-substituted purinyl and 8-aza-purinyl carbonucleosides based on indanol were synthesized from the commercially available (1R,2S)-1-amino-2-indanol and (1S,2R)-1-amino-2-indanol based on a well-known methodology.

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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 invention provides compounds of Formula I: 1wherein Azabicyclo is 23These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which alpha7 is known to be involved.

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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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Researchers are common within chemical engineering and are often tasked with creating and developing new chemical techniques, frequently combining other advanced and emerging scientific areas. Safety of 2,4-DimethylpyridineCatalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In an article, authors is Reitstoeen, Bjoern, once mentioned the new application about Safety of 2,4-Dimethylpyridine.

Cation radicals derived from anthracene and 9-substituted anthracenes react with pyridine and substituted pyridines to form pyridinium salts. 9-Nitro- and 9-cyano-substituted cation radicals were observed to be about 102 times as reactive as unsubstituted anthracene (AH) cation radicals while the 9-phenylanthracene (PAH) cation radical was found to be from 2 to 7 times less reactive than AH.+.The reactivities of the nitrogen-centered nucleophiles were observed to depend upon both electronic and steric factors.The mechanism of the reactions involves nucleophilic attack by the nitrogen lone pair at the 10-position of the cation radical.The reactions are accompanied by a change in hybridization, sp2 to sp3, at the anthracene 10-position, giving rise to inverse deuterium kinetic isotope effects ranging from 0.7 to 0.8 when the 10-position is substituted with deuterium.An electron-transfer mechanism for the substitution reactions was ruled out on the basis of energetic considerations.

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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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Van Soest fractionation is widely employed to characterize exogenous organic matter. The soluble fraction of Van Soest fractionation (SOL, extracted using hot water and then neutral detergent) often increases in line with compost maturity, although it is generally considered as labile. We have developed an alternative extraction method that comprises four successive steps (extraction using hot water, sodium tetraborate, dichloromethane/methanol and chelating resin) in order to clarify the chemical nature of the SOL fraction and explain its biodegradability. This method was tested on municipal solid waste compost sampled during the thermophilic phase (MSWi) and after 8months of composting (MSWm). Both methods extracted similar proportions of organic matter. The composition of the residues was similar in MSWm although differences were noted for the extraction of polysaccharides and lipids in the case of MSWi. The hot water extractable fraction decreased during composting. Its high biodegradability in MSWi was linked to the high polysaccharide content revealed by pyrolysis-GC/MS and FTIR spectroscopy. The increase in the sodium tetraborate extractable fraction mainly explained the increase in the SOL fraction during composting. This was made up of N-containing compounds, polysaccharides and lipids in the immature compost, and a majority of N-containing compounds in the mature compost. During composting, the stabilization of organic matter in the SOL fraction extractable by sodium tetraborate and EDTA might principally involve N-containing structures through the formation of complexes of organic matter with metal ions, especially Ca2+, which may be broken down during extraction of the Van Soest soluble fraction. These mechanisms still need to be investigated.

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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 chemically diverse library of secondary and tertiary 4-cyanomethyl-1,5-diphenyl-1H-pyrazole-3-carboxamides was synthesized to enable mapping of the SAR, in the eastern amide region, with regard to CB1 antagonist activity, This study was initiated as a prelude to the design and synthesis of possible CB1 antagonists that do not readily pass the blood-brain-barrier. In general a range of modifications were found to be tolerated in this part of the molecule, although polar and especially charged groups did to a degree reduce the CB1 antagonistic activity. Several compounds with single-digit or even sub-nanomolar potency, suitable for further elaboration of the nitrile moiety, were identified.

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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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Chemistry graduates have much scope to use their knowledge in a range of research sectors, including roles within chemical engineering, chemical and related industries, healthcare and more. Synthetic Route of 108-47-4, Name is 2,4-Dimethylpyridine, belongs to chiral-nitrogen-ligands compound, is a common compound. Synthetic Route of 108-47-4Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In an article, authors is Simonov, V. D., once mentioned the new application about Synthetic Route of 108-47-4.

By the reaction of perchloro-2-cyclopenten-1-one with pyridine and quinoline derivatives the corresponding onium salts of 2,4,4,5,5-pentachloro-3-hydroxy-2-cyclopentenone were obtained.The analogous reactions of perchloro-4-cyclopentene-1,3-dione lead either to onium salts of 2,2,5-trichloro-4-hydroxy-4-cyclopentene-1,3-dione or to betaines.The effect of the nature of the solvent and the structure of the amine on the reaction path was examined.

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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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Heats of ionization by thermometric titration for a series of bases (or acids) can be used to compare solid acids (or bases) with liquid analogues bearing the same functionalities in homogeneous solutions.The method is demonstrated for Broensted acids by reacting a series of substituted nitrogen bases with solutions of p-toluenesulfonic acid (PTSA) in acetonitrile and with suspensions of the microporous polymeric arylsulfonic acid resin-Dowex 50W-X8 in the same solvent.Under well-controlled anhydrous conditions there is a good correlation (r=0.992) between the heats of reaction of the bases with the homogeneous and heterogeneous acid systems, but the homogeneous system gives a more exothermic interaction by 3-4 kcal/mol for a series of 29 substituted pyridines, anilines, and some other amines.This difference may be attributed to homohydrogen bonding interactions between excess acid and sulfonate anion sites which are more restricted geometrically in the resin than in solution.Other factors which affect the enthalpy change for the acid-base interaction are the acid/base ratio, the water content of the sulfonic acid, the solvent, and the resin structure (e.g., microporous vs. macroporous).Steric hindrance in the base not differentiate solid from homogeneous acid.In addition to the use of titration calorimetry, heats of immersion are reported for the Dowex-arylsulfonic acid resins and the Nafion-perfluorinated sulfonic acid resin in a series of basic liquids.The results are compared with each other and with those from a previous study of several varieties of coal.

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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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Having gained chemical understanding at molecular level, name: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, belongs to chiral-nitrogen-ligands compound, is a common compound. name: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment. In an article, authors is Almasi, Diana, once mentioned the new application about name: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol.

Organocatalysts 1, derived from L-proline and (1S,2R)-cis-l-aminoindan-2-ol or (R)-l-aminoin-dane, are evaluated as promoters in the direct asymmetric aldol reaction between ketones and aromatic aldehydes in the presence of water and under solvent-free reaction conditions. L-Prolinethioamides 1c and 1d exhibited higher enantioselectivity than the corresponding prolinamides 1a and 1b in the model aldol reaction between cyclohexanone and 4-nitro-benzaldehyde in the presence of 4-nitrobenzoic acid as cocatalyst. In particular, L-prolinethioamide 1d (5 mol%), derived from L-proline and (R)-1-amino-indane, is shown as the most efficient organocatalyst studied promoting the direct aldol reaction of cyclo-alkyl, alkyl, and a-functionalized ketones with aromatic aldehydes in the presence of water and under solvent-free reaction conditions employing only 2 equivalents of nucleophile. Generally, anft-aldol products are obtained in high yields and excellent diastereo- and enantioselectivities (up to > 98/2 until syn, up to 98% ee). Solvent-free conditions give slightly higher dr and ee than using water as solvent. In addition, organocatalyst Id can be easily recovered by extractive work-up and reused. Prolinethio-amide Id (5 mol%) in combination with 4-NO2C6H4CO2H (5 mol%) is also a very effective or-ganocatalytic system for the asymmetric solvent-free intramolecular Haj os-Parrish-Eder-Sauer-Wiechert reaction with comparable or higher levels of enantioselectivity (up to 88% ee) to other reported catalysts in organic solvents.

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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 protocol for a practical and direct addition of alpha-and gamma-alkyl azaarenes to N-sulfonyl aldimines has been developed. Copper salts act as efficient Lewis acid catalysts for direct Mannich-type reactions providing a mild and fast access to various functionalized heterocycles.(Figure Presented)

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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