Top Picks: new discover of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE IN TREATING METABOLIC DISORDERS

The present invention provides compounds useful, for example, for modulating insulin levels in a subject, having the general formula I: wherein Q is an optionally substituted phenyl; L is a bond or O; P is a benzene or an optionally substituted thiazole ring; and R1 has the values provided herein. The present invention also provides compositions, uses, and methods for use of the compounds, for instance, for treatment of type II diabetes.

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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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Effect of micelle formation of quaternary pyridinium salts on their recyclization to anilines

The recyclization of N-alkyl-alpha-methylpyridinium salts with an N-alkyl chain consisting of 12 and 16 carbon atoms under the influence of aqueous solutions of sulfites of various amines was studied. It was established that the formation of micellar structures in aqueous solutions of these salts affects the direction of the reactions.

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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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Boronate urea activation of nitrocyclopropane carboxylates

Boronate ureas operate as catalysts for the activation of nitrocyclopropane carboxylates in nucleophilic ring-opening reactions. A variety of amines were found to open the urea-activated nitrocyclopropane carboxylates, generating highly useful nitro ester building blocks in good yields. Standard manipulations allow access to a wide range of valuable compounds from the ring-opened products with direct applications in bioactive target synthesis.

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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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Synthetic Route of 108-47-4, 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.108-47-4, Name is 2,4-Dimethylpyridine, molecular formula is C7H9N. In a article£¬once mentioned of 108-47-4

The Influence of Hydrogen Bonding on Diffusion II. Alcohol-Amine Systems in Carbon Tetrachloride

Measurements have been performed to learn about the influence of hydrogen bonding on the diffusion behaviour.Using the capillary method described by Anderson, the diffusion of benzyl alcohol and of trans-1-tert.butyl-4-cyclohexan-4-ol in CCl4 as a solvent has been measured, using IR-spectroscopy for the determination of the change of concentration as a function of time.In a second step, one aromatic amine was added to the solution and the analogous measurements have been repeated.It turned out that in this case the diffusion mobility of the alcohol molecules is lowered as a function of hydrogen bond strength. – Keywords: Diffusion of alcohols / Hydrogen bonding / Amines in the solvent

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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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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.In a patent, 108-47-4, name is 2,4-Dimethylpyridine, introducing its new discovery. Safety of 2,4-Dimethylpyridine

Superoxide dismutase activity of iron(II)TPEN complex and its derivatives

Superoxide is involved in the pathogenesis of various diseases, such as inflammation, ischemia-reperfusion injury and carcinogenesis. Superoxide dismutases (SODs) catalyze the disproportionation reaction of superoxide to produce oxygen and hydrogen peroxide, and can protect living cells against the toxicity of free radicals derived from oxygen. Thus, SODs and their functional mimics have potential value as pharmaceuticals. We have previously reported that Fe(II)tetrakis-N,N,N’,N’-(2-pyridylmethyl)ethylenediamine (Fe(II)TPEN) has an excellent SOD activity (IC50=0.5 muM) among many iron complexes examined (J. Biol. Chem., 264, 9243-9249 (1989)). Fe(II)TPEN can act like native SOD in living cells, and protect Escherichia coli cells from free radical toxicity caused by paraquat. In order to develop more effective SOD functional mimics, we synthesized Fe(II)TPEN derivatives with electron-donating or electron-withdrawing groups at the 4-position of all pyridines of TPEN, and measured the SOD activities and the redox potentials of these complexes. Fe(II) tetrakis-N,N,N’,N’-(4-methoxy-2-pyridylmethyl)ethylenediamine (Fe(II)(4MeO)4TPEN) had the highest SOD activity (IC50=0.1 muM) among these iron-based SOD mimics. In addition, a good correlation was found between the redox potential and the SOD activity of 15 Fe(II) complexes, including iron-based SOD mimics reported in the previous paper (J. Organometal. Chem., in press). Iron-based SOD mimics may be clinically applicable, because these complexes are generally tissue-permeable and show low toxicity. Therefore our findings should be significant for the development of clinically useful SOD mimics.

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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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P-Stereogenic Amino-Phosphines as Chiral Ligands: From Privileged Intermediates to Asymmetric Catalysis

ConspectusAmong chiral phosphines, P-stereogenic phosphines provide unparalleled activity and selectivity and have thus emerged as “state-of-the-art” ligands for asymmetric hydrogenation and other industrially relevant processes. However, the synthesis of this type of ligand implies lengthy multistep sequences, which are a hurdle for many laboratories. There is a lack of methods for the rapid construction of P-stereogenic phosphine ligands. In this respect, P-stereogenic synthons that can be rapidly incorporated into a given ligand scaffold are highly desirable. Over the last 10 years, our group has unveiled that P-stereogenic aminophosphines can be rapidly assembled in a convenient fashion from the corresponding primary aminophosphine and/or the corresponding phosphinous acid.Using cis-1-amino-2-indanol as chiral auxiliary, we devised a multigram synthesis of tert-butylmethylaminophosphine borane and tert-butylmethylphosphinous acid borane, which are key intermediate synthons. Primary aminophosphine works as nucleophilic intermediates at nitrogen. From this synthon, aminodiphosphine (MaxPHOS) and secondary imino phosphoranes (SIP) ligands were synthesized. These ligands exhibit a tautomeric equilibrium between the PH and NH forms, and because of that, they do not undergo oxidation in air. NH/PH tautomerism does not jeopardize their configurational stability, and most importantly, in the presence of a metal source, the equilibrium is shifted toward the NH form, thus allowing coordination through phosphorus. Rh-MaxPHOS and Rh-SIP complexes have been used in asymmetric hydrogenation and [2 + 2 + 2] cycloaddition reactions with outstanding results. On the other hand, P-stereogenic phosphinous acid, upon activation, serves as an electrophilic reagent with amine nucleophiles, allowing SN2 reactions at phosphorus with complete inversion of configuration. This coupling technology exhibits a great potential because it allows the incorporation of the P*-phosphine fragment in numerous ligand structures, provided there is an amino group with which to react. In a mild and efficient process, phosphinous acid has been coupled to hydrazine to yield C2 diphosphines and to chiral benzoimidazole-amines to yield P-stereogenic benzoimidazole-phosphine ligands. The most powerful ligand system, however, arises from the condensation of three independent fragments: Our phosphinous acid borane, an amino acid, and an amino alcohol, which yields a library of phosphino-oxazoline ligands named MaxPHOX. The corresponding Ir-MaxPHOX catalyst library was applied with excellent results in the asymmetric hydrogenation of alpha,beta-unsaturated esters, 2-aryl allyl phthalimides, unfunctionalized tetrasubstituted alkenes, cyclic enamides, and N-aryl and N-methyl imines. It also has found application in asymmetric isomerization of alkenes.Overall, we developed key P-stereogenic building blocks that can be incorporated stereospecifically to ligand scaffolds and demonstrated that integration of the P*-aminophosphine fragment in a given catalytic system provides structural diversity that can be a critical contribution to obtaining optimal results and selectivity.

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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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Simple synthesis of enantiomerically pure C2-symmetric bisoxazolidines from amino alcohols and formaldehyde

Treatment of chiral amino alcohols 1 with an excess of formaldehyde followed by reaction with NaOH at room temperature provides optically active C2-symmetric N,N’-methylenebisoxazolidines 2 in high 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

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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.In a patent, 108-47-4, name is 2,4-Dimethylpyridine, introducing its new discovery. SDS of cas: 108-47-4

Ferromagnetically Coupled Molecular Complexes with a CoII 2GdIII Pivalate Core: Synthesis, Structure, Magnetic Properties and Thermal Stability

New adducts with the composition [Co2Gd(NO3)(Piv)6L2] (L=2,4-lutidine (lut) (1), 2-phenylpyridine (PhPy) (4), 2-ethynylpyridine (EtPy) (5)) and [Co2Eu(NO3)(Piv)6(EtPy)2] (6) were synthesized. According to X-ray diffraction data, the molecular complexes comprise two atoms of cobalt(II) and one central atom of gadolinium(III) bridged by carboxylate ligands. The donor base molecules are coordinated to cobalt atoms. Magnetic measurements of the new and previously synthesized complexes with quinoline (2) and pyridine (3) ligands showed the ferromagnetic nature of the coupling between the metal centers in the CoII 2GdIII core with JCo-Gd parameters in the range of 0.15?0.18 cm?1. DFT calculations supported the ferromagnetic type of coupling for these complexes. Simultaneous thermal analysis of 1 and 2 showed the thermal stability of the complexes up to 180 C and the stepwise nature of thermolysis, which includes the stages of elimination of the donor base molecules and the thermal decomposition of the pivalate moieties in the complex.

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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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Enantioselective synthesis of an atropisomeric diaryl ether

(Chemical Equation Presented) Twisted ethers: Introduction of a bulky alkylsulfinyl substituent ortho to the C-O axis of a diaryl ether imposes a powerful conformational preference (see scheme). The preference persists upon oxidation of the sulfoxide to a sulfone, leading to dynamic thermodynamic resolution of the atropisomeric ether. This is the first enantioselective synthesis of an atropisomeric diaryl ether not forming part of a macrocyclic ring.

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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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Computational (MM, MD and MDMM) study of bidentate complexes of (R,R)- and meso-alpha,alpha?-bis(trifluoromethyl)-9,10-anthracenedimethanol with cis-1-amino-2-indanol

Results are reported from molecular mechanics (MM), molecular dynamics (MD) and a combined mode – MD with a subsequent MM minimization, of the complexes of the chiral solvating agent (CSA) alpha,alpha?-bis(trifluoromethyl)-9,10-anthracenedimethanol (1) in two of its diastereoisomeric forms ((R,R)- and meso-) with the substrates (1S,2R)- and (1R,2S)-cis-1-amino-2-indanol (2). Our computational work was stimulated by preceding NMR study of the enantio differentiation capacity of the CSA manifested in the formation of bidentate complexes with the substrates. The molecular modeling and simulation studies gave possible structures and relative stabilities of the associated species. MM minimizations were sufficient in order to find the lowest energy minima of meso-1/(1S,2R)-2 and (R,R)-1/(1S,2R)-2, while the lowest energy structure of (R,R)-1/(1R,2S)-2 was detected after the MD and MDMM studies. The complexes with the (R,R)-1 isomer have higher total energies than those with meso-1, in accord with an NMR estimate for longer lifetimes of the complexes with meso-1.

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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