Tag: 200-300

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 253168-94-4, Name is 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine. In a document, author is Niphade, Navnath C., introducing its new discovery. Quality Control of 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine.

Efficient and single pot process for the preparation of enantiomerically pure solifenacin succinate, an antimuscarinic agent

The development of an efficient and economic one-pot process, in which the configuration of the chiral centers of the starting materials is retained, for the preparation of highly pure solifenacin succinate, an antimuscarinic agent, is presented in this communication. The earlier reported processes suffer from the drawbacks of racemization and low yields due to the use of strong base, higher temperatures, and longer reaction times. The present work circumvents these issues by activating (3R)-quinuclidin-3-ol into a mixed active carbonate derivative by treating it with bis(4-nitrophenyl)carbonate. The subsequent reaction of the active carbonate with an enantiomerically pure amine without using any base at ambient temperature provided enantiomerically pure solifenacin with an overall yield of 90%.

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Related Products of 3564-73-6, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 3564-73-6, Name is 10,11-Dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, SMILES is O=C(N1C2=CC=CC=C2CCC3=CC=CC=C31)N, belongs to quinuclidines compound. In a article, author is Sadeghzadeh, Seyed Mohsen, introduce new discover of the category.

Quinuclidine Stabilized on FeNi3 Nanoparticles as Catalysts for Efficient, Green, and One-Pot Synthesis of Triazolo[1,2-a]indazole-triones

A new magnetically separable catalyst consisting of quinuclidin-3-thiol supported on propylsilane-functionalized silica-coated FeNi3 nanoparticles (FeNi3/quinuclidine) has been prepared. The synthesized catalyst was characterized by powder X-ray diffraction, transmission electron microscopy, vibrating sample magnetometry, thermogravimetric analysis, and Fourier transform infrared spectroscopy. The immobilized FeNi3/quinuclidine was shown to be an efficient heterogeneous catalyst for the synthesis of triazolo[1,2-a]indazole-triones under solvent-free conditions at room temperature. The catalyst is readily recovered by simple magnetic decantation and can be recycled several times with no significant loss of catalytic activity.

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 112-92-5, Name is 1-Hydroxyoctadecane, molecular formula is C18H38O. In an article, author is Suzuki, M,once mentioned of 112-92-5, SDS of cas: 112-92-5.

Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarcted rats

Solifenacin succinate [YM905, (+)-(1S,3′ R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] is a novel muscarinic receptor antagonist. We examined the effects of solifenacin and two other muscarinic receptor antagonists, tolterodine and propiverine, on detrusor overactivity in cerebral infarcted rats. Evaluation was done under conscious conditions using cystometry 1 day after middle cerebral artery occlusion. The cerebral infarcted rats showed decreases in bladder capacity and voided volume and an increase in residual volume, but no change in micturition pressure. Solifenacin increased bladder capacity and voided volume at doses of 0.03 mg/kg i.v. or more. Tolterodine increased bladder capacity and voided volume at 0.03 and 0.1 mg/kg i.v., while propiverine increased bladder capacity and voided volume at 1 mg/kg i.v. and at 0.3 and 1 mg/kg i.v., respectively. In contrast, none of the three drugs affected residual volume or micturition pressure. These results suggest that solifenacin may improve detrusor overactivity without causing urinary retention and may be a promising drug in the treatment of patients with overactive bladder syndrome. (c) 2005 Elsevier B.V. All rights reserved.

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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 3159-07-7, Name is 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine, molecular formula is C13H9NOS, belongs to quinuclidines compound, is a common compound. In a patnet, author is Prickaerts, Jos, once mentioned the new application about 3159-07-7, Application In Synthesis of 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine.

EVP-6124, a novel and selective alpha 7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of alpha 7 nicotinic acetylcholine receptors

EVP-6124, (R)-7-chloro-N-quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, is a novel partial agonist of alpha 7 neuronal nicotinic acetylcholine receptors (nAChRs) that was evaluated here in vitro and in vivo. In binding and functional experiments, EVP-6124 showed selectivity for alpha 7 nAChRs and did not activate or inhibit heteromeric alpha 4 beta 2 nAChRs. EVP-6124 had good brain penetration and an adequate exposure time. EVP-6124 (0.3 mg/kg, p.o.) significantly restored memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) in an object recognition task (ORT). Although donepezil at 0.1 mg/kg, p.o. or EVP-6124 at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory. In a natural forgetting test, an ORT with a 24 h retention time. EVP-6124 improved memory at 0.3 mg/kg, p.o. This improvement was blocked by the selective alpha 7 nAChR antagonist methyllycaconitine (0.3 mg/kg, i.p. or 10 mu g, i.c.v.). In co-application experiments of EVP-6124 with acetylcholine, sustained exposure to EVP-6124 in functional investigations in oocytes caused desensitization at concentrations greater than 3 nM, while lower concentrations (0.3-1 nM) caused an increase in the acetylcholine-evoked response. These actions were interpreted as representing a co-agonist activity of EVP-6124 with acetylcholine on alpha 7 nAChRs. The concentrations of EVP-6124 that resulted in physiological potentiation were consistent with the free drug concentrations in brain that improved memory performance in the ORT. These data suggest that the selective partial agonist EVP-6124 improves memory performance by potentiating the acetylcholine response of alpha 7 nAChRs and support new therapeutic strategies for the treatment of cognitive impairment. This article is part of a Special Issue entitled ‘Post-Traumatic Stress Disorder’. (C) 2011 Elsevier Ltd. All rights reserved.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 3159-07-7. The above is the message from the blog manager. Application In Synthesis of 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Recommanded Product: trans-Retinal, 116-31-4, Name is trans-Retinal, SMILES is O=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C, in an article , author is NILSSON, BM, once mentioned of 116-31-4.

3-HETEROARYL-SUBSTITUTED QUINUCLIDIN-3-OL AND QUINUCLIDIN-2-ENE DERIVATIVES AS MUSCARINIC ANTAGONISTS – SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS

A number of 3-heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives have been prepared and evaluated for muscarinic and antimuscarinic properties. The affinities of the new compounds (13, 14, 16-32, and 36-52a,b) were tested in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate [(-)-[H-3]QNB] as the radioligand and in a functional assay using isolated guinea pig urinary bladder. The present compounds behaved as competitive muscarinic antagonists in the urinary bladder. The highest receptor binding affinity, K-i (cortex) = 9.6 nM, was observed for 3-(2-benzofuranyl)quinuclidin-2-ene (31). The corresponding 3-benzofuranyl (36) and 3-benzothienyl (37) homologues had about 3.5-fold lower affinity for cortical muscarinic receptors. All quinuclidin-3-ol derivatives (14 and 16-25) had lower binding affinities for the different muscarinic receptor subtypes than the corresponding quinuclidin-2-ene analogues when examined in the various tissue homogenates. In general, the new compounds showed low subtype selectivity. The structure-affinity relationships are discussed in terms of differences in proton basicity of the azabicyclic nitrogen and differences in geometric, conformational, and/or electronic properties of the compounds. The cortical antimuscarinic potency is also related to the complementarity of the compounds to the putative binding site of the muscarinic mi receptor.

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Quinuclidine – Wikipedia,
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In an article, author is d’Agostino, Simone, once mentioned the application of 3564-73-6, HPLC of Formula: 238.28, Name is 10,11-Dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, molecular formula is C15H14N2O, molecular weight is 238.28, MDL number is MFCD00005072, category is quinuclidines. Now introduce a scientific discovery about this category.

Intriguing Case of Pseudo-Isomorphism between Chiral and Racemic Crystals of rac- and (S)/(R)2-(1,8-Naphthalimido)-2-quinuclidin-3-yl, and Their Reactivity Toward I-2 and 1Br

Condensation reactions between 1,8-naphthalic anhydride and racemic 3-aminoquinuclidine or chiral (S) or (R)-(-)-3-aminoquinuclidine allowed preparation of three novel racemic and enantiopure aza-donor ligands, namely NMiABCO (1), (S)NMiABCO (2a), and (R)NMiABCO (2b). Racemic NMiABCO (1) crystallizes in the monoclinic space group P2(1)/c, Z’ = 1, while enantiopure (S)NMiABCO (2a) and (R)NMiABCO (2b) crystallize in the chiral monoclinic space group P2(1), Z’ = 2, and show significant pseudocentrosymmetry, being pseudo-isomorphous with racemic NMiABCO (1). Reactivity of both racemic and enantiopure NMiABCO toward iodine and interhalogen IBr was also investigated as a way to remove the pseudoisomorphism, yielding the three new molecular adducts [NMiABCO center dot I-2] (3), [(S)NMiABCO center dot I-2]center dot xCHCl(3) (4), [(S)NMiABCO center dot IBr]center dot xCHCl(3) (5) and the molecular salt [HNMIABCO][1Br(2)] (6). Synthesis of complexes 3 and 4 was also carried out in the solid state via kneading and vapor digestion techniques. All compounds were fully characterized via single crystal and powder X-ray diffraction and Raman spectroscopy.

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Quinuclidine – Wikipedia,
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Chemistry is an experimental science, Recommanded Product: 6753-98-6, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 6753-98-6, Name is (1E,4E,8E)-2,6,6,9-Tetramethylcycloundeca-1,4,8-triene, molecular formula is C15H24, belongs to quinuclidines compound. In a document, author is Primozic, I.

Interactions of chiral quinuclidin-3-yl benzoates with butyrylcholinesterase: kinetic study and docking simulations

Both enantiomers of quinuclidin-3-yl benzoate (RQBz and SQBz) were synthesized in order to examine the stereoselectivity of the hydrolysis of these esters catalyzed by horse serum butyrylcholinesterase (BChE). The hydrolysis of benzoylcholine (BzCh) was also studied in order to determine the influence of the alcohol part of the esters upon the kinetics. The k(cat) value for the substrates decreased in order BzCh > RQBz (4-fold slower) much greater than SQBz (76-fold slower reaction). K-M values determined for quinuclidinium substrates revealed that the binding affinity of RQBz (0.28 mm) is approximately 2-fold lower than that of SQBz (0.13 mM) towards BChE. From the ratio of the enantiomeric k(cat)/K-M values, an enantiomeric excess of 78% was calculated, indicating that the resolution of racemic quinuclidin-3-yl benzoate can be achieved by hydrolysis with BChE. The orientations of all the studied benzoate esters and butyrylcholine (BuCh) in the active site of human BChE were proposed by flexible ligand docking with AutoDock 3.0. Analyses of the Michaelis complexes obtained revealed that there are numerous similar close contacts in the active site. The main difference in binding of quinuclidinium and choline esters was found in the ammonium electrostatic region which includes cation-pi interaction of the ammonium moiety of substrates with the indole ring of Trp(84). The important cation-pi interaction with Trp(84) was lowest in the case of the S-enantiomer of QBz, which might be the main explanation for the slowest rate of hydrolysis of that compound. Copyright (C) 2002 John Wiley Sons, Ltd.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 6753-98-6. Recommanded Product: 6753-98-6.

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Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , COA of Formula: 284.4357, 116-31-4, Name is trans-Retinal, molecular formula is C20H28O, belongs to quinuclidines compound. In a document, author is Radl, S, introduce the new discover.

Synthesis and antinociceptive activity of some 3-chlorophenyl- and 6-chloropyridin-2-yl derivatives

Derivatives of 2-chloro-6-(4-hydroxy-1-methylpiperidin-4-yl)pyridine (2b) were prepared and tested as analgesics. 2-Chloro-6-lithiopyridine treated with quinuclidin-3-one, 1-methylpyrrolidin-3-one, 2-(dimethylaminomethyl) cyclohexanone, and ethyl 1-methylpiperidin-4-ylcarboxylate provided the corresponding alcohols 5, 6, 13a, and 6-chloro-2-pyridyl 1l-methylpiperidin-4-yl ketone (9). The ketone was reduced with sodium borohydride or treated with methylmagnesium chloride or phenyllithium to provide the corresponding alcohols 11, 12a and 12b, respectively. 1-[4-(6-Chloro-2-pyridyl)1-methyrpiperidin-4-yl]1-methylethanol (4b) was prepared from 2-chloro-6-(1-methyl-1,2,5,6-tetrahydropyridin-4-yl)pyridine (14b) by treatment with butyllithium and acetone followed by reduction of intermediate 15b with sodium cyanoborohydride.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 116-31-4. COA of Formula: 284.4357.

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Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , Formula: 239.27, 51997-51-4, Name is 4-Glycidyloxycarbazole, molecular formula is C15H13NO2, belongs to quinuclidines compound. In a document, author is Madadi, Nikhil Reddy, introduce the new discover.

Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel, high affinity ligands for CB1 and CB2 cannabinoid receptors

A small library of N-benzyl indolequinuclidinone (IQD) analogs has been identified as a novel class of cannabinoid ligands. The affinity and selectivity of these IQDs for the two established cannabinoid receptor subtypes, CB1 and CB2, was evaluated. Compounds 8 (R = R-2 = H, R-1 = F) and 13 (R = COOCH3, R-1 = R-2 = H) exhibited high affinity for CB2 receptors with K-i values of 1.33 and 2.50 nM, respectively, and had lower affinities for the CBI receptor (K-i values of 9.23 and 85.7 nM, respectively). Compound 13 had the highest selectivity of all the compounds examined, and represents a potent cannabinoid ligand with 34-times greater selectivity for CB2R over CB1R. These findings are significant for future drug development, given recent reports demonstrating beneficial use of cannabinoid ligands in a wide variety of human disease states including drug abuse, depression, schizophrenia, inflammation, chronic pain, obesity, osteoporosis and cancer. (C) 2013 Elsevier Ltd. All rights reserved.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 51997-51-4. Formula: 239.27.

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, 105-50-0, Name is Diethyl 1,3-acetonedicarboxylate, SMILES is O=C(OCC)CC(CC(OCC)=O)=O, belongs to quinuclidines compound. In a document, author is Boskovic, Perica, introduce the new discover, Safety of Diethyl 1,3-acetonedicarboxylate.

The Aggregation Behavior and Antioxidative Activity of Amphiphilic Surfactants Based on Quinuclidin-3-ol

The self-aggregation and thermodynamic properties of three cationic quaternary ammonium surfactants were investigated. The physicochemical properties of compounds containing quinuclidin-3-ol with even number of carbon atoms (10, 12, and 14) in the hydrophobic tail were measured by conductivity, dynamic light scattering (DLS), and Zeta-potential measurements. DLS and Zeta-potential measurements show a similar size distribution for all surfactants with excellent uniformity, and Zeta-potential increases significantly with increase in the size of hydrocarbon tail. The critical micelle concentration (CMC) and the degree of micelle ionization (beta) were determined using conductivity measurements. The CMC values of surfactants were found to be between 3.4 and 23.8 x 10(-3) M. The standard Gibbs free energy (Delta Gmico) was derived from conductivity measurements and suggests that surfactants containing longer chains spontaneously form micelles. The antioxidative properties of these cationic surfactants were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) assays. Among the tested samples, N-tetradecyl-3-hydroxyquinuclidinium bromide (QOH-C14) exhibited the highest antioxidative potential (388.30 nmol (TE) equivalents mL(-1)), which was further investigated by the DNA nicking assay.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 105-50-0 is helpful to your research. Safety of Diethyl 1,3-acetonedicarboxylate.

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