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V1A RECEPTOR AGONISTS

Compounds of formula (I), salts thereof, and compositions and uses thereof are described. The compounds are useful as V1a vasopressin agonists, for the treatment of, e.g., complications of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.

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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

More research is needed about 108-47-4

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Regioselectivity in free radical bromination of unsymmetrical dimethylated pyridines

During a literature review some curious inconsistencies in the free radical bromination of picolines were noted. To achieve a better understanding of the mechanisms and regioselectivity we reran these reactions, extending our work to unsymmetrical lutidines using N-bromosuccinimide in limiting amount. Characterization of the products was done with GC/MS and H NMR. The regioselectivity of bromination in unsymmetrical dimethylpyridines shows that nitrogen in the ring is deactivating inductively. The competition between 2,3, 2,4, and 2,5 dimethyl pyridine toward bromination results with bromination in the methyl group farthest from the N in the ring. 3,4-Lutidine shows only the 4,4-dibrominated product.

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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 2,4-Dimethylpyridine

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One-pot synthesis of indolizine via 1,3-dipolar cycloaddition using a sub-equivalent amount of K2Cr2O7 as an efficient oxidant under base free conditions

A one-pot method for synthesizing multi-substituted indolizines from alpha-halo-carbonyl compounds, pyridines and electron deficient alkenes was developed. A sub-equivalent amount of potassium dichromate was used as an oxidant under base free conditions. The transformation developed should be of economic efficiency.

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

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Microwave-assisted synthesis of n-heterocycles and their evaluation using an acetylcholinesterase immobilized capillary reactor

Polarized ketene dithioketals have been recognized as useful building blocks in many synthetic operations. In this work, a transition-metal-free annulations of 1,1-bis(thiomethyl)-2-nitroethylene with hydroxylalkylamines or alkyldiamines have been reported. This methodology provides a directed approach to N-heterocycles, e.g., imidazolidines, oxazolidines and benzoxazoles under microwave conditions. These compounds were evaluated as acetylcholinesterase inhibitors by using an enzyme immobilized capillary reactor-tandem mass spectrometry.

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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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A mild and efficient H2O2 oxygenation of N-heteroaromatic compounds to the amine N-oxides and KI deoxygenation back to the tertiary amine with hexaphenyloxodiphosphonium triflate

A mild and efficient method for the oxidation of N-heteroaromatic compounds to the corresponding N-oxides using H2O2 in the presence of hexaphenyloxodiphosphnium triflate (Hendrickson reagent) in EtOH at room temperature was reported. This methodology presented relatively fast and selective reactions to afford the N-oxides in good yields. The reverse reactions, deoxygenation reactions, were also carried out under the same reaction conditions by KI to produce the tertiary amines.

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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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Bisphenol compound composition having excellent thermal stability

The purpose of the invention is to improve thermal stability of bisphenol compounds.The resolving means of the invention is to include a pyridine compound in bisphenol compounds.

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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

A new application about (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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Rhodium(I) complexes containing beta-amino alcohol and 1,2-diamine ligands: Syntheses, structures, and catalytic applications

The bridge-opening reaction of [(eta4-C8H 12)2Rh2(mu-Cl)2] with chiral and achiral beta-amino alcohol nucleophiles gave mononuclear complexes [(eta4-C8H12)RhCl(HN(R)?OH-kappaN)] containing the amino alcohol ligands in N-monodentate coordination; HN(R)?OH = ethanolamine (4), 2-amino-2-methyl-1-propanol (5), and either enantiomer of (R)-, (S)-2-amino-3-methyl-1-butanol (D-, L-valinol) [(R)-6, (S)-6], (R)-, (S)-2-pyrrolidinemethanol (D-, L-prolinol) [(R)-7, [S)-7], (1S,2R)-, (1R,2S)-2-amino-1-phenyl-1-propanol (D-, L-norephedrine) [(1S,2R)-8, (1R,2S)-8], and (1S.2R)-, (1R,2S)-cis-1-amino-2-indanol [(1S,2R)-9, (1R,2S)-9], Coordination of the free hydroxy function of the N,O ligands was brought about by both dehydrochlorination, which furnished the neutral valinolato chelate complex [(eta4-C8H12)Rh{(S)-H 2NCH(CHMe2)CH2O-kappaN,kappaO}], (S)-10, and by precipitation of the metal-bound chloride with TlO3SCF 3 to produce ionic chelate complexes [(eta4-C 8H12)Rh(HN(R)?OH-kappaN,kappaO}]O 3SCF3; HN(R)?OH = 2-amino-2-methyl-1-propanol (11), (S)-2-amino-3-methyl-1-butanol [(S)-12], (S)-2-pyrrolidinemethanol [(S)-13], (IR,2S)-2-amino-1-phenyl-1-propanol [(1R,2S)-14], and (1R,2S)-cis-1-amino-2- indanol [(1R,2S)-15]. Except for only two in situ characterized [{(R)-binap}Rh(H2N?OH-kappaN,kappaO)]+ cations, where H2N?OH = L-valinol or L-norephedrine, no compound containing the various N,O ligands in addition to mono- or bidentate phosphanes could be prepared. In contrast, the P2/N2-coordinated chelate complexes [{(R)-binap}Rh-(H2N?NH2)]BF 4 with H2N?NH2 = H2NCMe 2CMe2NH2 [(R)-(16)], (R,R)-H 2NCH(Ph)CH(Ph)NH2 [(R),(R,R)-17], and (R,R)-1,2-(H 2N)2C6H10 [(R),(R,R)-18] were easily obtained from [(eta4-C8H12)Rh{(R)-binap}] BF4 and 1,2-diamines. Oxidative addition of HCl to (R),(R,R)-17 produced trans-[{(R)-binap}-Rh(H)(Cl){(R,R)-H2NCH(Ph)CH(Ph)NH 2}]BF4 [(R),(R,R)-19], If activated by strong base (KOH), (R),(R,R)-17 and (R),(R,R)-19 acted as moderately active and enantioselective catalysts for the reduction of acetophenone by both direct and transfer hydrogenation: eemax: 71% (S). The crystal structures of 4, (S)-6, (R)-7, (1R,2S)-8, (S)-10, (1R,2S)-14, (1R,2S)-15, (R)-16, (R),(R,R)-17, and two alcohol/alcoholato addition compounds, [(eta4-C8H 12)Rh(H2NCMe2CH2O-kappaN,kappaO) ][(eta4-C8H12)Rh(H2-NCMe 2CH2OH-kappaN,kappaO)][(eta4-C 8H12)RhCl2] [1-2], and [(eta4- C8H12)Rh(H2NCMe2CH 2O-kappaN,kappaO)][(eta4-C8H 12)Rh(H2-NCMe2CH2OH-kappaN, kappaO)]Cl [1-3], were determined. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.

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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 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Recommanded Product: 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 119139-23-0, in my other articles.

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Development of a Kilogram-Scale Synthesis of a Novel MC1R Agonist

Herein, we report the kilogram-scale synthesis of CD08108, a novel MC1R agonist. This synthesis has been developed to produce the first batches of this compound for preclinical and clinical studies. Two amido couplings were used to synthesize the backbone of the API. Improvements have been made to isolate crystalline intermediates and to remove all column chromatographic steps. Crystallization of the final API was monitored by DSC in-process control during slurry ripening of the amorphous suspension of the hydrochloride salt.

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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

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