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POLYMORPHIC FORM OF A TACHYKININ RECEPTOR ANTAGONIST

This invention is concerned with a novel polymorphic forms of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethyl-amino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl) morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethylamino)methyl-1, 2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

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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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Lewis acid promoted benzylic cross-couplings of pyridines with aryl bromides

Either ZnCl2, Sc(OTf)3, or BF3OEt 2 can promote the palladium-catalyzed arylation of methylpyridines and related heterocycles (see example). The complexation of the Lewis acid to the nitrogen atom in the heterocycle facilitates the reductive elimination, leading to various arylated pyridines in high yields. BF3OEt 2 was also found to promote highly regioselective metalations in the case of 2,4-lutidine. Copyright

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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

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

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HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: Improved antiviral activity in cells

By a small modification in the core structure of the previously reported series of HIV-1 protease inhibitors that encompasses a tertiary alcohol as part of the transition-state mimicking scaffold, up to 56 times more potent compounds were obtained exhibiting EC50 values down to 3 nM. Three of the inhibitors also displayed excellent activity against selected resistant isolates of HIV-1. The synthesis of 25 new and optically pure HIV-1 protease inhibitors is reported, along with methods for elongation of the inhibitor P1? side chain using microwave-accelerated, palladium-catalyzed cross-coupling reactions, the biological evaluation, and X-ray data obtained from one of the most potent analogues cocrystallized with both the wild type and the L63P, V82T, I84 V mutant of the HIV-1 protease.

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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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108-47-4, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum. 108-47-4, Name is 2,4-Dimethylpyridine, molecular formula is C7H9N. In a Article£¬once mentioned of 108-47-4

POTENTIOMETRIC STUDIES ON COMPLEXES OF SILVER(I) IN SOLUTIONS. PART V. RELATIONSHIP BETWEEN STABILITY CONSTANTS OF Ag(I) COMPLEXES OF PYRIDINE DERIVATIVES AND HAMMET’S ? COEFFICIENTS

By means of the potentiometric method, the processes of formation of Ag(I) complexes of 3-acetyl-, 3-hydroxymethyl-, 2-ethyl-, 2,4-dimethyl-, 2,4,6-trimethyl-, 2-amino-5-methyl-, and 2-amino-4-methylpyridines have been examined in aqueous solutions (I = 0.5 (KNO3), t = 25 deg C).Correlation has been found between pKa and stability coefficient Sf and substituent constants ? for 19 Ag(I) compounds with 3- and 4-substituted pyridine derivatives.Positive value of the slope of Sf = f(?) straight line dependence evidences that the contribution of ?M -> L bond in the metal-ligand co-ordination bond is considerable.

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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

Discovery of C9H11NO

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In homogeneous catalysis, catalysts are in the same phase as the reactants. Chemistry is traditionally divided into organic and inorganic chemistry. Recommanded Product: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In an article£¬Which mentioned a new discovery about 126456-43-7

Lipase-mediated resolution of trans-1-azidoindan-2-ol: A new route to optically pure cis-1-aminoindan-2-ol

Optically pure trans-1-azidoindan-2-ol has been prepared in both enantiomeric forms via lipase-mediated kinetic transesterification in organic solvent. A route to optically pure cis-1-aminoindan-2-ol has also been developed by using the optically pure trans-azidoalcohol thus obtained.

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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

Extracurricular laboratory:new discovery of C7H9N

The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research.Recommanded Product: 2,4-Dimethylpyridine, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 108-47-4, in my other articles.

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Phenol-Amine Hydrogen Bonds with Large Proton Polarizabilities. Position of the OH…N<*>O(1-)…H(1+)N Equilibrium as a Function of the Donor and Acceptor

1:1 mixtures of octylamine+chlorophenols and pentachlorophenol+aromatic amines have been studied in CCl4 solution using infrared spectroscopy.It has been shown by conductivity measurements that no charged species are present in these systems.Therefore only the association constants Ka, and the equilibrium constants, KPT, of proton transfer in the equilibrium OH…N<*>O(1-)…H(+)N need be considered.Linear relations exist between log Ka and the DeltapKa values for both families of systems.Log KPT increases with both systems in proportion to DeltapKa, i.e. the Huyskens equation is valid.This increase is caused by a decrease in the enthalphy term DeltaH<*>0 due to increasing acidities of the donors or (in the other family of systems) increasing basicities of the acceptors.In addition to this direct effect, an increase in the size of the negative DeltaH<*>I values due to the increasing interaction of these hydrogen bonds with their environment is responsible for this shift in the equilibrium. DeltapK50percenta amounts to 3.6 in the case of the family containing the aliphatic amine and 1.6 in the case of the family containing the aromatic amines, since with the latter the charge is spread over a more extended region if the proton approaches the N atom.The intensity of the continuum (and thus the proton polarizability) is largest if both proton-limiting structures OH…N and O(1-)…H(1+)N have almost the same probability.

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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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In homogeneous catalysis, catalysts are in the same phase as the reactants. Chemistry is traditionally divided into organic and inorganic chemistry. Quality Control of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In an article£¬Which mentioned a new discovery about 126456-43-7

Enantioselective synthesis of densely functionalized pyranochromenes via an unpredictable cascade Michael-oxa-Michael-tautomerization sequence

A surprising example of enantioselective cascade Michael-oxa-Michael- tautomerization reactions of malononitrile and benzylidenechromanones has been developed. In this case, malononitrile functions as both nucleophile and electrophile. Meanwhile, a simple bifunctional indane amine-thiourea catalyst has been discovered to promote this process to afford high yields (up to 99%) and high to excellent enantiomeric excesses (81-99% ee). Copyright

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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 108-47-4

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In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. Application In Synthesis of 2,4-Dimethylpyridine, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.108-47-4, name is 2,4-Dimethylpyridine. In an article£¬Which mentioned a new discovery about 108-47-4

Simultaneous abatement of diesel soot and NOX emissions by effective catalysts at low temperature: An overview

The diesel engine generally achieves the highest fuel, energy, and thermal efficiency due to its very high compression/expansion ratio (14:1 to 25:1). Diesel engines can have a thermal efficiency that exceeds 50%. The main problem is that they emit more pollution like fine black soot particulates (C8H to C10H) and nitrogen oxides (NOX). These pollutants have been causing serious problems for human health and the global environment and also impacts on the engine. There are many types of catalysts investigated for simultaneous control of these two pollutants, i.e., platinum group metals (PGM; Pt, Pd, Rh, and Ir) based, spinel-type oxides, hydrotalcite, rare earth metal oxides, mixed transient metal oxides, etc. The high raw material cost of PGM catalysts has become a significant issue, so developing non-PGM catalysts are one of the promising challenges. There are no extra reductants required because soot catalytically oxidizes itself in the presence of NOX at a faster rate than molecular oxygen and simultaneously NOX is reduced to nitrogen. The order of oxidation potential of NOX to oxidized soot in comparison to molecular oxygen is as follows: NO2?>?NO?>?O2. To meet the very strict EPA US 2010 and Euro VI regulations of particulate matter (PM) and NOX for heavy-duty and light-duty vehicular stringent emission, it is very important to apply the integrated catalytic systems to significantly remove PM and NOX simultaneously. Many papers related to simultaneous control of soot and NOX over different catalysts have been published but till now some of effective catalysts showing high conversion at low temperatures (possibly within the range typical of diesel exhaust: 150?450C) have not been reviewed. Thus, this article provides a summary of published information regarding the effective catalysts, their preparation methods, properties, and application for simultaneous control of diesel soot and NOX.

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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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Activation of free-radical polyfluoroalkylation of organic substrates with freon BrCF2CF2Br using a system of organic base-electron transfer mediator

A polyfluoroalkylation of pyrrole and phenols with freon BrCF2CF2Br using sulfur dioxide-substituted pyridine activating system proceeds at the aromatic nucleus by a free-radical mechanism. The essential influence of the basicity of the medium is demonstrated and 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

Top Picks: new discover of C9H11NO

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Convenient method for the preparation of carbamates, carbonates, and thiocarbonates

(Chemical Equation Presented) A convenient, rapid, and efficient method for the preparation of carbamates from amines with 1-alkoxycarbonyl-3-nitro-1,2,4- triazole transfer reagents is reported. Reactions of newly synthesized stable crystalline reagents with alkyl amines were completed in a few minutes without any additional base, and highly pure carbamates were obtained without chromatographic purification. These highly active reagents are also useful for the selective protection of nucleobases and preparation of carbonates and thiocarbonates.

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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