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Rigid aminoalcohol backbone as a highly defined chiral template for the preparation of optically active tertiary alpha-hydroxyl acids

Constrained aminoalcohol derived-ketoester or amides have provided a new entry for the production of enantiopure acid 1 for (S)-oxybutynin.

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

New explortion of 2,4-Dimethylpyridine

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Deuterium Nuclear Magnetic Resonance Spectroscopy. II. Distribution of Deuterium in some Labelled Nitrogen Heterocyclic Compounds

Pyridine, methylpyridines, quinoline and isoquinoline have been labelled with deuterium using pre-reduced platinum dioxide (PtO2*2H2O) and heavy water.Their 2H chemical shifts from monodeuteriated TMS have been assigned.The extent of the labelling has been determined directly by 2H NMR spectroscopy.

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

Properties and Exciting Facts About 108-47-4

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Geometries and tautomerism of OHN hydrogen bonds in aprotic solution probed by H/D isotope effects on 13C NMR chemical shifts

The 1H and 13C NMR spectra of 17 OHN hydrogen-bonded complexes formed by CH313COOH(D) with 14 substituted pyridines, 2 amines, and N-methylimidazole have been measured in the temperature region between 110 and 150 K using CDF3/CDF2Cl mixture as solvent. The slow proton and hydrogen bond exchange regime was reached, and the H/D isotope effects on the 13C chemical shifts of the carboxyl group were measured. In combination with the analysis of the corresponding 1H chemical shifts, it was possible to distinguish between OHN hydrogen bonds exhibiting a single proton position and those exhibiting a fast proton tautomerism between molecular and zwitterionic forms. Using H-bond correlations, we relate the H/D isotope effects on the 13C chemical shifts of the carboxyl group with the OHN hydrogen bond geometries.

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

Can You Really Do Chemisty Experiments About 126456-43-7

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HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: An investigation into the role of the P1′ side chain on structure-activity

A systematic investigation was undertaken to determine the role of the P1′ sidechain in a series of hydroxyethylene isostere based inhibitors of HIV-1 protease. Substitution and homologation of the benzyl P1′ side chain of the Phe-Phe isostere based pseudo peptides 1 (L-682,679) and 2 (L-685,434) with various heteroalkyl groups leads to a series of extremely potent inhibitors of the enzyme. Several examples of the most potent inhibitors were very effective in an ex vivo cell based viral spread assay using human H9 T- lymphocytes and the IIIb isolate of HIV-1. Compound 19 is 120 times more potent than 1 and 16 times more potent than 2 in inhibiting the spread of infection in this assay.

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

Archives for Chemistry Experiments of 2,4-Dimethylpyridine

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Studies on antiulcer drugs. V. Synthesis and antiulcer activity of aralkylbenzazoles

A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H2-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H2-receptor antagonist activity in contrast to imidazo[1,2-a]pyridine analogues (I). On antiulcer assay, however, some pyridine derivatives (II) exerted higher activity than the reference compounds, sofalcone, sucralfate and cimetidine. The structure activity relationships of these compounds are discussed.

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

Archives for Chemistry Experiments of 126456-43-7

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A chiral three tooth nitrogenphosphine oxygen ligand and its related biligand in asymmetric catalytic application of the catalyst in the reaction (by machine translation)

The present invention relates to a class of tridentate ligands and related ligand PNHO in asymmetric hydrogenation and its similar application of the catalyst in the reaction. The present invention discloses a novel three nitro phosphine oxygen ligand is the 1st example of the ferrocene-containing plane under nitro phosphine oxygen ligand, and successfully applied to is simple an aromatic ketone, alpha? Hydroxy ketone, beta? Ketoesters efficient high selective asymmetric hydrogenation reaction and the like. A tridentate ligands compared with other advantages, the synthetic route of ligand of this type is extremely simple, low cost, easy large-scale synthesis, air stable, the asymmetric hydrogenation of the carbon-oxygen double bond reaction demonstrate the high activity and high selectivity. (by machine translation)

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

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Thermochemical Comparisons of Homogeneous and Heterogeneous Acids and Bases. 1. Sulfonic Acid Solutions and Resins as Prototype Broensted Acids

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£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Brief introduction of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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Chemically modified mutant serine hydrolases show improved catalytic activity and chiral selectivity

This invention provides novel chemically modified mutant serine hydrolases that catalyze a transamidation and/or a transpeptidation and/or a transesterification reaction. The modified serine hydrolases have one or more amino acid residues in a subsite replaced with a cysteine, wherein the cysteine is modified by replacing the thiol hydrogen in the cysteine with a substituent group providing a thiol side chain comprising a moiety selected from the group consisting of a polar aromatic substituent, an alkyl amino group with a positive charge, and a glycoside. In particularly preferred embodiments, the substitutents include an oxazolidinone, a C1 to C15 alkyl amino group with a positive charge, or a glycoside.

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

Simple exploration of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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Thiourea Derivative of 2-[(1 R)-1-Aminoethyl]phenol: A Flexible Pocket-like Chiral Solvating Agent (CSA) for the Enantiodifferentiation of Amino Acid Derivatives by NMR Spectroscopy

Thiourea derivatives of 2-[(1R)-1-aminoethyl]phenol, (1S,2R)-1-amino-2,3-dihydro-1H-inden-2-ol, (1R,2R)-(1S,2R)-1-amino-2,3-dihydro-1H-inden-2-ol, and (R)-1-phenylethanamine have been compared as chiral solvating agents (CSAs) for the enantiodiscrimination of derivatized amino acids using nuclear magnetic resonance (NMR) spectroscopy. Thiourea derivative, prepared by reacting 2-[(1R)-1-aminoethyl]phenol with benzoyl isothiocyanate, constitutes an effective CSA for the enantiodiscrimination of N-3,5-dinitrobenzoyl (DNB) derivatives of amino acids with free or derivatized carboxyl functions. A base additive 1,4-diazabicyclo[2.2.2]octane(DABCO)/N,N-dimethylpyridin-4-amine (DMAP)/NBu4OH) is required both to solubilize amino acid derivatives with free carboxyl groups in CDCl3 and to mediate their interaction with the chiral auxiliary to attain efficient differentiation of the NMR signals of enantiomeric substrates. For ternary systems CSA/substrate/DABCO, the chiral discrimination mechanism has been ascertained through the NMR determination of complexation stoichiometry, association constants, and stereochemical features of the diastereomeric solvates.

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

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The application of HETPHOX ligands to the intramolecular asymmetric Heck reaction

A new thiophene-oxazoline P,N ligand derived from cis-aminoindanol was prepared and a range of analogous HETPHOX ligands were applied to the intramolecular Heck reaction. The enantioselectivity obtained was 76% employing the tert-butyl-substituted HETPHOX ligand with an aryl triflate spirooxindole precursor. The isomer distribution of the product spirooxindoles was high (up to 99:1). Georg Thieme Verlag Stuttgart.

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