A new application about 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione

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Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.

We previously reported the discovery of several spirodiketopiperazine derivatives as potent CCR5 antagonists with anti-HIV activity. Herein, we describe in detail the identification of these lead compounds using a combinatorial chemistry approach. A novel spirodiketopiperazine scaffold was designed on the basis of the concept of the privileged structure of G-protein-coupled receptors (GPCRs). This new framework was obtained in acceptable yield with high purity from the readily prepared isonitrile resin through the Ugi reaction, sequential transformations, and cyclative cleavage. By measuring the inhibitory activity of each compound in the initial library against the intracellular calcium mobilization stimulated by MIP-1alpha, several compounds were found to show modest but selective CCR5 antagonistic activity. After the rapid evaluation of these hit compounds, several single-digit nanomolar, low-molecular-weight CCR5 antagonists that can potently block the infectivity and replication of laboratory and clinical strains of HIV as well as those of highly drug-resistant HIV variants with minimal cytotoxicity have been identified.

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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 126456-43-7

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Scale-up of flow-assisted synthesis of C2-symmetric chiral PyBox ligands

A series of PyBox ligands were prepared from commercially available chelidonic acid by a multistep flow sequence using mesoreactor technology. A chloro group introduced onto the ligand scaffold was subsequently exploited to give amine derivatives ready for immobilization through microencapsulation technologies. Georg Thieme Verlag Stuttgart ¡¤ New York.

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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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Experimental and theoretical study of the kinetic of proton transfer reaction by ion mobility spectrometry

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 ¡Á 10-9, 0.90 ¡Á 10-9 and 0.68 ¡Á 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£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

Brief introduction of 2,4-Dimethylpyridine

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Reference of 108-47-4, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 108-47-4, Name is 2,4-Dimethylpyridine, molecular formula is C7H9N. In a Patent£¬once mentioned of 108-47-4

BICYCLOSULFONYL ACID (BCSA) COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-a Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-a, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in

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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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Development of a novel fluorine-18 labeled deuterated fluororasagiline ([18F]fluororasagiline-D2) radioligand for PET studies of monoamino oxidase B (MAO-B)

The objective of this study was to synthesize and evaluate a novel fluorine-18 labeled deuterium substituted analogue of rasagiline (9, [ 18F]fluororasagiline-D2) as a potential PET radioligand for studies of monoamine oxidase B (MAO-B). The precursor compound (6) and reference standard (7) were synthesized in multi-step syntheses. Radiolabeling of 9 was accomplished by a two-step synthesis, compromising a nucleophilic substitution followed by hydrolysis of the sulfamidate group. The incorporation radiochemical yield from fluorine-18 fluoride was higher than 30%, the radiochemical purity was >99% and the specific radioactivity was >160 GBq/mumol at the time of administration. In vitro compound 7 inhibited the MAO-B activity with an IC50 of 173.0 ¡À 13.6 nM. The MAO-A activity was inhibited with an IC50 of 9.9 ¡À 1.1 muM. The fluorine-18 version 9 was characterized in the cynomolgus monkey brain where a high brain uptake was found (275% SUV at 4 min). There was a higher uptake in the striatum and thalamus compared to the cortex and cerebellum. A pronounced blocking effect (50% decrease) was observed in the specific brain regions after administration of l-deprenyl (0.5 mg/kg) 30 min prior to the administration of 9. Radiometabolite studies demonstrated 40% of unchanged radioligand at 90 min post injection. An efficient radiolabeling of 9 was successfully established and in the monkey brain 9 binds to MAO-B rich regions and its binding is blocked by the selective MAO-B compound l-deprenyl. The radioligand 9 is a potential candidate for human PET studies.

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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 2,4-Dimethylpyridine

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Catalytic Direct-type 1,4-Addition Reactions of Alkylazaarenes

1,4-addition reactions of alkylazaarenes catalyzed by strong Br¡ãnsted bases have been developed for the first time. The desired reactions with alpha,beta-unsaturated amides proceeded under mild reaction conditions to give the 1,4-adducts in high yields. Both ortho- and para-substituted azaarenes afforded the desired adducts in high yields. Regioselective reactions of di- or trimethylpyridine were found to be possible depending on the acidity of the alpha-hydrogen atoms. Furthermore, a candidate of allosteric protein kinase modulators was synthesized in two steps. An asymmetric variant of this reaction was also found to be feasible.

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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 2,4-Dimethylpyridine

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Synthesis and Decomposition Kinetic Studies of Bis(lutidine)silver(I) Nitrate Complexes as an Interdisciplinary Undergraduate Chemistry Experiment

Interdisciplinary experiments are being offered in upper-division chemistry laboratory courses in an attempt to encourage students to make a connection between techniques learned in one discipline to affirm chemical principles that form the basis of chemical reactions in another chemistry discipline. A new interdisciplinary experiment is described in which students synthesize bis(lutidine)silver(I) nitrate complexes, where the position of the methyl groups on the pyridine ring varies. The stability of these metal complexes is evaluated as a function of basicity of the ligand by studying the rate of decomposition of the metal complex through isothermal thermogravimetric analysis. An Arrhenius plot is used to determine activation energies for the decomposition reaction, and the data are used to establish the positive correlation between the activation energy with the basicity of the lutidine ligand.

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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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Process for the separation of a mixture of enantiomers

A diastereomer complex obtained via a process for the separation of enantiomers is disclosed, wherein separation can be rapidly effected such that enantiomers are obtained with high e.e. values. The process pets the separation of mixtures of enantiomers in which more than one resolving agent is used, of which at least one resolving agent is optically active, and which yields a diastereomer complex containing at least two resolving agents in optically active form. The process provides for, inter alia, a diastereomer complex having at least three compounds of which at least two compounds are resolving agents in optically active form, and at least one compound is an onantiomer in optically active form. Also provided is a diastereomer complex having at least three compounds of which at lea one compound is a resolving agent in optically active form, and at least two compounds which are enantiomers in optically active form.

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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 2,4-Dimethylpyridine

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THE INTERACTION OF ELECTROPHILIC SILANES (Me3SiX, X= ClO4, I, CF3SO3, Br, Cl) WITH NUCLEOPHILES. THE NATURE OF SILYLATION MIXTURES IN SOLUTION.

Silanes, Me3SiX, and Nucleophiles, Nu, form 1:1 salts, Me3SiNu(1+)*X(1-) in solution.The effect of both nucleophile and silane on salt formation has been studied, and the implications for the design of more efficient silylation mixtures are 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

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

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Stereoselective synthesis of P-stereogenic aminophosphines: Ring opening of bulky oxazaphospholidines

A highly diastereoselective and efficient synthesis of P-stereogenic bulky alkyl and aryl aminophosphines that relies on ring opening of tert-butyl-oxazaphospholidine 2 is described. Ring opening with several organometallic reagents takes place with inversion of configuration at the phosphorus center as it has been demonstrated by X-ray analysis of two ring-opened intermediates. The unprecedented reactivity observed is attributed to the presence of a free NH functionality that facilitates the attack of the organometallic reagent in an SN2@P-type process.

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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