Discovery of (S)-Bis(3,5-bis(trifluoromethyl)phenyl)(pyrrolidin-2-yl)methanol

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Inhibitors of phosphodiesterase type 5A for treating or preventing muscle disease or the symptoms thereof in a patient

Disclosed are pharmaceutical compositions and methods for treating or preventing muscle diseases or the symptoms thereof. The compositions typically include and the methods typically utilize phosphodiesterase type 5A inhibitors.

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Top Picks: new discover of 137076-54-1

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Chemistry is traditionally divided into organic and inorganic chemistry. name: 2-(4,7,10-Tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 137076-54-1

Radiometal-Dependent Biological Profile of the Radiolabeled Gastrin-Releasing Peptide Receptor Antagonist SB3 in Cancer Theranostics: Metabolic and Biodistribution Patterns Defined by Neprilysin

Recent advances in oncology involve the use of diagnostic/therapeutic radionuclide-carrier pairs that target cancer cells, offering exciting opportunities for personalized patient treatment. Theranostic gastrin-releasing peptide receptor (GRPR)-directed radiopeptides have been proposed for the management of GRPR-expressing prostate and breast cancers. We have recently introduced the PET tracer 68Ga-SB3 (SB3, DOTA-p-aminomethylaniline-diglycolic acid-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-NHEt), a receptor-radioantagonist that enables the visualization of GRPR-positive lesions in humans. Aiming to fully assess the theranostic potential of SB3, we herein report on the impact of switching 68Ga to 111In/177Lu-label on the biological properties of resulting radiopeptides. Notably, the bioavailability of 111In/177Lu-SB3 in mice drastically deteriorated compared with metabolically robust 68Ga-SB3, and as a result led to poorer 111In/177Lu-SB3 uptake in GRPR-positive PC-3 xenografts. The peptide cleavage sites were identified by chromatographic comparison of blood samples from mice intravenously receiving 111In/177Lu-SB3 with each of newly synthesized 111In/177Lu-SB3-fragments. Coinjection of the radioconjugates with the neprilysin (NEP)-inhibitor phosphoramidon led to full stabilization of 111In/177Lu-SB3 in peripheral mouse blood and resulted in markedly enhanced radiolabel uptake in the PC-3 tumors. In conclusion, in situ NEP-inhibition led to indistinguishable 68Ga/111In/177Lu-SB3 profiles in mice emphasizing the theranostic prospects of SB3 for clinical use.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.name: 2-(4,7,10-Tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid, you can also check out more blogs about137076-54-1

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Awesome Chemistry Experiments For 52093-25-1

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Computed Properties of C3EuF9O9S3, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 52093-25-1, Name is Europium(III) trifluoromethanesulfonate, molecular formula is C3EuF9O9S3. In a Article, authors is Gunnlaugsson, Thorfinnur£¬once mentioned of 52093-25-1

Synthesis, structural and biological evaluation of GlyAla based lanthanide macrocyclic conjugates as supramolecular ribonuclease mimics

The glycine-alanine conjugated ligands of cyclen (1,4,7,10,-tetraazacyclododecane) 1 and 2, possessing methyl and benzyl alanine esters respectively, and the corresponding lanthanide complexes 1La, 1Eu, 1Tb, 1Yb, 2La, 2Eu, and 2Tb were designed with the aim of mimicking the nature of the hydrophobic cavity of ribonucleases. X-ray crystallographic investigations showed that 2Tb has a typical monocapped square antiprism geometry, where the Tb(III) ion is central, coordinating to the four amino moieties of the cyclen ring and four of the oxygens of amide carbonyl groups of the glycine residues of the four pendant arms, with the ninth coordinated site being occupied by a water molecule. All the complexes were shown to promote the hydrolysis of the phosphodiester bond of 2-hydroxypropyl p-nitrophenyl phosphate (HPNP, tau1/2 = 5.78 ¡Á 103 h) with 1Tb being the most efficient in promoting such hydrolysis at pH 7.4 and at 37 C for the 1Ln family with tau1/2 = 4.9 h. For the 2Ln family, 2La was most effective in promoting hydrolysis of HPNP, with tau1/2 = 3.7 h. The rate of hydrolysis was also investigated for 1La and 2La as function of pH, with both complexes displaying bell-shaped pH dependence within the physiological pH range. For 1Ln the highest activity was observed at pH 7.0, with tau1/2 = 4.6 h, whereas for 2La it occurred at pH 7.4. Beyond pH 8, the rate of both complexes was shown to be almost linearly increased. The ability of 1Eu and 2Eu to cleave a 23-mer sequence from the mRNA of the GAG-HIV gene was also investigated. It was found that both gave rise to cleavage of the sequence at every nucleotide residue after 4 h of incubations at pH 7.4 and 37 C.

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Properties and Exciting Facts About Cerium(III) trifluoromethanesulfonate

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Aldehydes vs aldimines. Unprecedented aldimine-selective nucleophilic additions in the coexistence of aldehydes using a lanthanide salt as a Lewis acid catalyst

It is well-recognized that aldimines are less reactive than aldehydes toward nucleophilic additions. In this paper, an unprecedented change in the reactivity is described: preferential reactions of aldimines over aldehydes in nucleophilic additions using a lanthanide salt as a Lewis acid catalyst. In the presence of a catalytic amount of ytterbium triflate (Yb(OTf)3), only aldimines reacted with silyl enol ethers, ketene silyl acetals, allyltributylstannane, or cyanotrimethylsilane to afford the corresponding adducts in high yields, even in the coexistence of aldehydes. Selective formation of an aldimine-Yb(OTf)3 complex rather than an aldehyde-Yb(OTf)3 complex was indicated by 13C NMR analyses. While this report demonstrates the effective use of Lewis acids in organic synthesis, the basic idea of changing reactivity as shown here will be widely applied to many other nucleophilic additions.

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Metal catalyst and ligand design,
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A new application about Europium(III) trifluoromethanesulfonate

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Related Products of 52093-25-1, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 52093-25-1, Name is Europium(III) trifluoromethanesulfonate,introducing its new discovery.

Synthesis, stereocontrol and structural studies of highly luminescent chiral tris-amidepyridyl-triazacyclononane lanthanide complexes

The configuration of the remote amide chiral moiety determines the helicity of the metal complex in Ln(iii) complexes of nonadentate N6O 3 ligands based on triazacyclononane. Solution NMR studies revealed the presence of a dominant isomer whose proportion varies from 9:1 to 4:1 from Ce to Yb and X-ray crystallographic studies at 120 K of the Yb and two enantiomeric Eu complexes confirmed the configuration as S-Delta-lambda in the major isomer. Global minimisation methods allowed magnetic susceptibility and electronic relaxation times of the lanthanide ions to be estimated by analysis of variable field longitudinal relaxation rate (R1) data sets. A set of four europium complexes, containing different para-substituted pyridinyl-aryl groups, exist as one major isomer (15:1), and absorb light strongly via an ICT transition in the range 320 to 355 nm (epsilon = 55 to 65000 M-1 cm-1). The two examples absorbing light at 332 nm, possess overall emission quantum yields of 35 and 37% in aerated water, making these systems as bright as any Eu complex in solution. This journal is the Partner Organisations 2014.

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Metal catalyst and ligand design,
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A new application about Europium(III) trifluoromethanesulfonate

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A promising change in the selection of the circular polarization excitation used in the measurement of Eu(III) circularly polarized luminescence

A judicious change in the selected transition used for circular polarization excitation will overcome the low oscillator strength limitation of the currently allowed magnetic-dipole 5Di ? 7F 2 (Eu(III)) transition chosen for circularly polarized luminescence (CPL) measurement. The proposed allowed magnetic-dipole 5Di ? 7F0 (Eu(III)) transition will facilitate the detection of CPL from the Eu(III) systems of interest. CPL on the acetonitrile solution of the chiral tris complex of Eu(III) with (R,R)N,N?–bis(1-phenylethyl)-2,6- pyridinedicarboxamide ([Eu((R,R)-1)3]3+), recently suggested as an effective and reliable CPL calibrating agent, confirms the feasibility of the proposed experimental procedure. A comparable CPL activity exhibited by the acetonitrile solution of [Eu((R,R)-1)3]3+ following direct excitation in the spectral range of the 5D 1 ? 7F0 transition and upon indirect excitation through the ligand absorption bands (lambdaexc = 308 nm) was observed. This confirms that the recommended magnetic-dipole allowed absorption transition, 5Di ? 7F0, is the transition to be considered in the measurement of CPL. This work provides critical direction for the continued instrumental improvements that can be done for developing CPL into a biomolecular structural probe.

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Metal catalyst and ligand design,
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Awesome and Easy Science Experiments about 76089-77-5

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, HPLC of Formula: C3CeF9O9S3, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 76089-77-5, Name is Cerium(III) trifluoromethanesulfonate, molecular formula is C3CeF9O9S3. In a Article, authors is Fiorito, Serena£¬once mentioned of 76089-77-5

Ytterbium triflate promoted solvent-free synthesis of 2-amino-4H-pyranes

2-Amino-4H-pyrane derivatives are nowadays well recognized as valuable scaffold in drug discovery. In this manuscript a new and improved multicomponent process for the chemical synthesis of the title compounds is described. beta-Dicarbonyl and activated cyanomethylene compounds, and aromatic, aliphatic or alpha,beta-unsaturated aldehydes have been subjected to a three-component reaction under the catalysis of ytterbium triflate hydrate under solvent-free conditions at 50?C, and by application of microwaves and ultrasounds. Of the three methodologies employed, the reaction in neat performed in a flask with magnetic stirring proved to be by far the most efficient, providing the desired adducts in very good yields (85?91%). The experimental protocol set-up in this study was applied without significant differences in terms of yields to aromatic aldehydes having electron withdrawing or electron-donating substituents, as well as to aliphatic and alpha,beta-unsaturated ones. Moreover ytterbium triflate has been easily recovered from each reaction media and reused without appreciable loss of its catalytic activity.

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Extended knowledge of Cerium(III) trifluoromethanesulfonate

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Controlled hydrolysis of lanthanide complexes of the N-donor tripod tris(2-pyridylmethyl)amine versus bisligand complex formation

The reaction of the lanthanide salts LnI3(thf)4 and Ln(OTf)3 with tris(2-pyridylmethyl)amine (tpa) was studied in rigorously anhydrous conditions and in the presence of water. Under rigorously anhydrous conditions the successive formation of mono- and bis(tpa) complexes was observed on addition of 1 and 2 equiv of ligand, respectively. Addition of a third ligand equivalent did not yield additional complexes. The mono(tpa) complex [Ce(tpa)l3] (1) and the bis(tpa) complexes [Ln(tpa) 2]X3 (X = I, Ln = La(III) (2), Ln = Ce(III) (3), Ln = Nd(III) (4), Ln = Lu(III) (5); X = OTf, Ln = Eu(III) (6)) were isolated under rigorously anhydrous conditions and their solid-state and solution structures determined. In the presence of water, 1H NMR spectroscopy and ES-MS show that the successive addition of 1-3 equiv of tpa to triflate or iodide salts of the lanthanides results in the formation of mono(tpa) aqua complexes followed by formation of protonated tpa and hydroxo complexes. The solid-state structures of the complexes [Eu(tpa)(H2O)2(OTf) 3] (7), [Eu(tpa)(mu-OH)(OTf)2]2 (8), and [Ce(tpa)(mu-OH)(MeCN)(H2O]2I4 (9) have been determined. The reaction of the bis(tpa) lanthanide complexes with stoichiometric amounts of water yields a facile synthetic route to a family of discrete dimeric hydroxide-bridged lanthanide complexes prepared in a controlled manner. The suggested mechanism for this reaction involves the displacement of one tpa ligand by two water molecules to form the mono(tpa) complex, which subsequently reacts with the noncoordinated tpa to form the dimeric hydroxo species.

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Some scientific research about 137076-54-1

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ Safety of 2-(4,7,10-Tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid, Which mentioned a new discovery about 137076-54-1

Synthesis and evaluation of a monoreactive DOTA derivative for indium-111-based residualizing label to estimate protein pharmacokinetics

The purpose of this study was to develop an indium-111 (111In)-based residualizing label for estimating the pharmacokinetics of proteins. 1,4,7,10-Tetraazacyclododecane-N,N?,N?,N?-tetraacetic acid (DOTA), which produced a highly stable and hydrophilic 111In chelate, was selected as the chelating site, and the monoreactive DOTA derivative with a tetrafluorophenyl group as the protein binding site (mDOTA) was designed to avoid cross-linkings of proteins. mDOTA was synthesized with an overall yield of 11%. The stability in murine plasma, the radioactivity retention in the catabolic sites of proteins and the radiochemical yields of 111In-labelled proteins via mDOTA were investigated using human serum albumin (HSA), galactosyl-neoglycoalbumin (NGA) and cytochrome c (cyt c) as model proteins. 111In-labelled HSA via mDOTA was highly stable for 5 days after incubation in murine plasma. Long retention of radioactivity in the catabolic sites was observed after injection of 111In-DOTA-NGA in mice, due to the slow elimination of the radiometabolite from the lysosome. At a chelator concentration of 42.2 muM, 111In-DOTA-cyt c was produced with over 91 % radiochemical yield. On the other hand, 111In-DOTA-lysine and 111In-DOTA were obtained with high radiochemical yields at lower chelator concentrations. These findings indicated that mDOTA would be an appropriate 111In-labelling agent for estimating protein pharmacokinetics. These findings also suggested that the introduction of a protein binding site at a position distal from the unmodified DOTA structure would be preferable to preparing 111In-DOTA-labelled proteins with higher specific activity.

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Metal catalyst and ligand design,
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Awesome Chemistry Experiments For (S,S)-(+)-N,N’-Bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine

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Synthetic Route of 135616-36-3, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 135616-36-3, Name is (S,S)-(+)-N,N’-Bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine,introducing its new discovery.

Synthesis and in vivo evaluation of [18F]UCB-J for PET imaging of synaptic vesicle glycoprotein 2A (SV2A)

Purpose: Synaptic abnormalities have been implicated in a variety of neuropsychiatric disorders, including epilepsy, Alzheimer?s disease, and schizophrenia. Hence, PET imaging of the synaptic vesicle glycoprotein 2A (SV2A) may be a valuable in vivo biomarker for neurologic and psychiatric diseases. We previously developed [11C]UCB-J, a PET radiotracer with high affinity and selectivity toward SV2A; however, the short radioactive half-life (20 min for 11C) places some limitations on its broader application. Herein, we report the first synthesis of the longer-lived 18F-labeled counterpart (half-life: 110 min), [18F]UCB-J, and its evaluation in nonhuman primates. Methods: [18F]UCB-J was synthesized from the iodonium precursors. PET imaging experiments with [18F]UCB-J were conducted in rhesus monkeys to assess the pharmacokinetic and in vivo binding properties. Arterial samples were taken for analysis of radioactive metabolites and generation of input functions. Regional time?activity curves were analyzed using the one-tissue compartment model to derive regional distribution volumes and binding potentials for comparison with [11C]UCB-J. Results: [18F]UCB-J was prepared in high radiochemical and enantiomeric purity, but low radiochemical yield. Evaluation in nonhuman primates indicated that the radiotracer displayed pharmacokinetic and imaging characteristics similar to those of [11C]UCB-J, with moderate metabolism rate, high brain uptake, fast and reversible binding kinetics, and high specific binding signals. Conclusion: We have accomplished the first synthesis of the novel SV2A radiotracer [18F]UCB-J. [18F]UCB-J is demonstrated to be an excellent imaging agent and may prove to be useful for imaging and quantification of SV2A expression, and synaptic density, in humans.

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