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HIV protease inhibitors having polyether substituents

[From equivalent EP0487270A2] Polyether derivatives of the form, A-G-B-B-J psi wherein G is a dipeptide isostere substituted with a polyether, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of DIV 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£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 (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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Electric Literature of 126456-43-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.126456-43-7, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, molecular formula is C9H11NO. In a Article£¬once mentioned of 126456-43-7

Facile synthesis of a chiral urea bridged bisoxazoline ligand and structural characterization of its bis-copper(ii)-chloride complex

A facile synthesis of a new bisoxazoline ligand is described. This ligand contains a urea bridging unit and is capable of stabilizing bimetallic complexes. An X-ray crystal structure of a bis-copper complex is reported.

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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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Development of a scalable synthesis of a GPR40 receptor agonist

Early process development and salt selection for AMG 837, a novel GPR40 receptor agonist, is described. The synthetic route to AMG 837 involved the convergent synthesis and coupling of two key fragments, (S)-3-(4-hydroxyphenyl) hex-4-ynoic acid (1) and 3-(bromomethyl)-4?-(trifluoromethyl)biphenyl (2). The chiral beta-alkynyl acid 1 was prepared in 35% overall yield via classical resolution of the corresponding racemic acid (¡À)-1. An efficient and scalable synthesis of (¡À)-1 was achieved via a telescoped sequence of reactions including the conjugate alkynylation of an in situ protected Meldrum’s acid derived acceptor prepared from 3. The biaryl bromide 2 was prepared in 86% yield via a 2-step Suzuki-Miyaura coupling-bromination sequence. Chemoselective phenol alkylation mediated by tetrabutylphosphonium hydroxide allowed direct coupling of 1 and 2 to afford AMG 837. Due to the poor physiochemical stability of the free acid form of the drug substance, a sodium salt form was selected for early development, and a more stable, crystalline hemicalcium salt dihydrate form was subsequently developed. Overall, the original 12-step synthesis of AMG 837 was replaced by a robust 9-step route affording the target in 25% yield.

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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

Final Thoughts on Chemistry for 126456-43-7

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Application of 126456-43-7, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.126456-43-7, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, molecular formula is C9H11NO. In a article£¬once mentioned of 126456-43-7

Synthesis and General Biological Activity of a Small Adenosine-5?-(Carboxamide and Sulfanilamide) Library

A small library of fifty-five adenosine peptide analogs was synthesized, under the Pilot Scale Library (PSL) Program of the NIH Roadmap initiative, from 2?,3?-O-isopropylideneadenosine-5?-carboxylic acid 2. The coupling of amine or sulfanilamide reactants to the free 5?-carboxylic acid moiety of 2, in automated solution-phase fashion, led after acid-mediated hydrolysis to target compounds 3-57 in good yields and high purity. No marked anticancer or antimalarial activity was noted on preliminary cellular testing. Initial screening through the MLPCN program, however, indicates that these analogs may show diverse and interesting biological activities.

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

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Electric Literature of 126456-43-7, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.126456-43-7, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, molecular formula is C9H11NO. In a article£¬once mentioned of 126456-43-7

Heterocycles with a Stereogenic Phosphorus or Sulfur Atom Derived from Aminoalcohols or Aminonaphthols

This chapter presents the synthesis of heterocycles with a stereogenic phosphorus or sulfur atom derived from aminoalcohols or aminonaphthols, which has been reported recently (usually after 2002). It also contains selected references to the earlier papers and is divided into three sections, describing methods of synthesis of the three particular classes of heterocyclic derivatives. The first two are devoted to heterocycles with a stereogenic phosphorus atom and discuss the protocols for the preparation of 1,3,2-oxazaphospholanes (1,3,2-oxazaphospholidines) with a tri- and tetracoordinated phosphorus atom, 1,3,2-oxazaphosphorinanes and larger rings containing a stereogenic phosphorus atom forming part of the nitrogen-phosphorus-oxygen (NPO) grouping. The third section concerning heterocycles with a stereogenic sulfur atom describes the synthesis of all kinds of 1,2,3-oxathiazolidine 2-oxides and tetrahydro-1,2,3-oxathiazine-2-oxides.

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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

Final Thoughts on Chemistry for 108-47-4

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A review of inhibitors for the corrosion of transition metals in aqueous acids

The importance of the electrical double layer at the interface between a metal and an acid electrolyte together with its interaction with organic and inorganic molecules to produce initially electrostatic adsorption are highlighted. In some cases, a chemical bond is formed involving charge transfer or charge sharing between the metal surface and inhibitor molecules forming a coordinate bond through lone-pair electrons on heteroatoms or pi electrons on inhibitors with multiple and aromatic bonds. The application of mathematical formulae to the variation in adsorbed inhibitor molecules at the metal surface is considered, with inhibitor concentration isotherms considering thermodynamic principles or the water displacement reaction where for an inhibitor molecule to adsorb at a metal surface several water molecules must be displaced first. The predominant ways in which molecules enable inhibition are formation of a physical barrier where a physical adsorbed barrier of molecules (usually polymeric or oxide promoting for this mode to predominant) impede movement near the metal surface or reduction in metal reactivity where chemisorbed inhibitor molecules adhere to active sites on the metals reducing the number of cathodic and anodic sites. Adsorption involving charged inhibitor species causes a change in the double layer and the potential at the outer Helmholtz plane, influencing the corrosion rates of both anodic and cathodic reactions. The first three modes are intimately with adsorption and the double layer the last involves interaction of the inhibitor molecules and the intermediate products formed during the partial electrochemical reactions, interaction of the adsorbed intermediates with organic molecules can either decrease (inhibit) or increase (stimulate) electrode reaction rate depending on the stability of the inhibitor-intermediate complex formed.

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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

Some scientific research about (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. category: chiral-nitrogen-ligands, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 126456-43-7, name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol. In an article£¬Which mentioned a new discovery about 126456-43-7

Palladium-Catalyzed Amide-Directed Enantioselective Hydrocarbofunctionalization of Unactivated Alkenes Using a Chiral Monodentate Oxazoline Ligand

A Pd-catalyzed amide-directed enantioselective hydrocarbofunctionalization of unactivated alkenes with C-H nucleophiles has been developed using a chiral monodentate oxazoline (MOXin) ligand. Various indoles react at C3 position with aminoquinoline-coupled 3-alkenamides to give gamma addition products in good to excellent yield and enantioselectivity. This study represents an important advance of the development of chiral monodentate oxazoline ligands, which have been underexplored for asymmetric catalysis.

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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 2,4-Dimethylpyridine

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Retention of ionizable compounds in high-performance liquid chromatography 14. Acid-base pK values in acetonitrile-water mobile phases

Linear relationships between sspKa values in acetonitrile-water mixtures and wwpKa values in pure water have been established for five families of compounds: aliphatic carboxylic acids, aromatic carboxylic acids, phenols, amines, and pyridines. The parameters (slope and intercept) of the linear correlations have been related with acetonitrile-water composition. The proposed equations allow accurate estimation of the pKa values of any member of the studied families at any acetonitrile-water composition up to 60% of acetonitrile in volume (100% for pyridines). Conversely, the same equations can be used to estimate aqueous pKa values from chromatographic pKa values obtained from any acetonitrile-water mobile phase between the composition range studied. Estimation of pKa values have been tested with chromatographic literature data.

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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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PREPARATION AND CATALYTIC ACTIVITY OF CATIONIC RHODIUM TETRAFLUOROBENZOBARRELENE COMPLEXES WITH NITROGEN AND PHOSPHORUS DONOR LIGANDS

The preparation and properties of twenty five new cationic rhodium(I) complexes with tetrafluorobenzobarrelene and mono- or bidentate nitrogen or phosphorus donor ligands are described.The complexes with tertiary phosphines show high selectivities in the hydrogenation of 1-hexyne and several diolefins towards monoolefins.The dependence of the reduction rate upon the basicity of the phosphine has been studied.

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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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Tertiary Alcohols as Radical Precursors for the Introduction of Tertiary Substituents into Heteroarenes

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£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