Simple exploration of C9H11NO

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Low nanomolar corticotropin releasing factor type-1 (CRF1) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a Ki = 11 ± 1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine.

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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 compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson’s Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

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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. category: chiral-nitrogen-ligands, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, belongs to chiral-nitrogen-ligands compound, is a common compound. category: chiral-nitrogen-ligandsCatalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In an article, authors is Duffy, Joseph L., once mentioned the new application about category: chiral-nitrogen-ligands.

Transposition of the pyridyl nitrogen from the P3 substituent to the P1? substituent in HIV-1 protease inhibitors (PI) affords compounds such as 3 with an improved inhibitory profile against multiple P450 isoforms. These compounds also displayed increased potency, with 3 inhibiting viral spread (CIC95) at <8 nM for every strain of PI-resistant HIV-1 tested. The poor to modest bioavailability of these compounds may correlate in part to their aqueous solubility. The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research.category: chiral-nitrogen-ligands, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 126456-43-7, in my other articles.

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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By tethering of a polar hydrophilic group to the P1 or P1′ substituent of a Phe-based hydroxyethylene isostere, the antiviral potency of a series of HIV protease inhibitors was improved. The optimum enhancement of anti-HIV activity was observed with the 4-morpholinylethoxy substituent. The substituent effect is consistent with a model derived from inhibitor docked in the crystal structure of the native enzyme. An X-ray crystal structure of the inhibited enzyme determined to 2.25 A verifies the modeling predictions.

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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

Top Picks: new discover of 2,4-Dimethylpyridine

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Rate constants of the proton transfer reactions RH+ + DMP ? R + DMP·H+, where R was acetone (Ac), trimethyl amine (TMA) or H2O and DMP was 2,4-dimethyl pyridine have been measured by ion mobility spectrometry (IMS). The Reactant R was injected into the ionization region of IMS to produce RH+ while DMP was continuously delivered to the drift region to react with the RH+ pulsed into the drift tube by a shutter grid. Since DMP.H+ was generated along the drift tube, a tail appeared in the IMS spectrum that contained kinetic information. To prevent proton-bound dimer formation, the reactions were carried out at elevated temperatures (170-230 C). We measured rate constants of 1.17 × 10-9, 0.90 × 10-9 and 0.68 × 10-9 cm3 s-1 for proton transfer from H3O +, Ac·H+ and TMA·H+ to DMP, respectively. The experimental rate constants were almost temperature independent, indicating that no activation energy was involved in those proton transfer reactions. The rate constants were also calculated by using average dipole orientation (ADO) theory at B3LYP and MP2 levels. The calculated values revealed acceptable agreement between the experimental and theoretical trends. 2014 Elsevier B.V.

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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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Pd-catalyzed decarboxylative cross-couplings of 2-(2-azaaryl)acetates with aryl halides and triflates have been discovered. This reaction is potentially useful for the synthesis of some functionalized pyridines, quinolines, pyrazines, benzoxazoles, and benzothiazoles. Theoretical analysis shows that the nitrogen atom at the 2-position of the heteroaromatics directly coordinates to Pd(II) in the decarboxylation transition state.

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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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Various N-<(2-haloaryl)methyl>pyridinium, N-(arylmethyl)-2-halopyridinium and N-(2-halobenzyl)isoquinolinium salts have been synthesized and their intramolecular photocyclization reactions studied.Upon irradiation the aqueous solution of N-<(2-haloaryl)methyl>pyridinium and N-arylmethyl-2-halopyridinium salts 1, 2 were cyclized to give isoindolium salts.In contrast to the pyridinium salts 1, 2, the aqueous solution of N-(2-halobenzyl)isoquinolinium salts 3 appear not to undergo photocyclization.N-Benzyl-2-chloropyridinium salts 1c is more reactive than N-(2-chlorobenzyl)pyridinium salt 1a in the photocyclization.N-(2-Chlorobenzyl)-2-chloropyridinium salt 1d is three times more reactive than 1c.A mechanism of ?-complex formation of the halogen moiety of the pyridinium ring with the phenyl ring is suggested for the reactive pyridinium salt.The triplet energy of the isoquinolinium salts 3 is too low to photocyclize.

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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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Strong Br°nsted-base-catalyzed addition reactions of alkylazaarenes with vinylsilanes are reported. The reactions of alkylpyridines and their analogues with vinylsilanes proceed in moderate to high yields in the presence of catalytic amounts of LiTMP, LiCl, and MS 4A. This is a general method that can be applied to catalytic addition reactions of alkylazaarenes with vinylsilanes.

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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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Low dielectric constant apolar aprotic solvents, although employed on a limited scale for studying proton transfer reactions as compared with commonly used polar protic or dipolar aprotic ones, offer some particular advantages, namely, specific solute?solvent interactions are virtually eliminated and proton transfer occurs directly in an apolar aprotic solvent. An intriguing feature of these reactions is their general acid-catalyzed/base-catalyzed kinetics with a time scale over microseconds to minutes. In fact, the true or intrinsic relative strengths of acids/bases when measured in such solvents come to the fore much more clearly than those obtained in other classes of solvents. Recently, a review documenting the post-1980 developments relating to proton transfer reactions in apolar aprotic solvents has been published. The present article is a commentary of the pre-1980 developments in this area since the 1920s Br°nsted?Lowry’s ?proton cult? of acid?base theory. Copyright

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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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Condensation of alpha-methylpyridinium, quinolinium and isoquinolinium salts with 1,2-dicarbonyls in the presence of base, yielded quinolizinium derivatives.In an analogous process, alpha-benzyl derivatives produced 2,3-dihydroindolizin-2-ones by intramolecular cyclisation.

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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