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Reference of 119139-23-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 119139-23-0, molcular formula is C20H13N3O2, introducing its new discovery.

BENZIMIDAZOLYL-METHYL UREA DERIVATIVES AS ALX RECEPTOR AGONISTS

The present invention relates to benzimidazolyl-methyl urea derivatives of formula (I), wherein n, D, E, R1, R2, R3, R4, R6, R7, R8 and R9 are as defined in the description, their preparation and their use as pharmaceutically active 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

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NOVEL PHTHALAZINONE-PYRROLOPYRIMIDINECARBOXAMIDE DERIVATIVES

The compounds of formula (1) in which R1, R7, R8, R9, R10, R17, R18, R19, R20 and m have the meanings as given in the description, are novel effective inhibitors of type 4 and type 5 phosphodiesterase.

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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

Awesome and Easy Science Experiments about 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione

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119139-23-0, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 119139-23-0, name is 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione. In an article£¬Which mentioned a new discovery about 119139-23-0

Total Synthesis of Cryptophycins-1, -3, -4, -24 (Arenastatin A), and -29, Cytotoxic Depsipeptides from Cyanobacteria of the Nostocaceae

A convergent synthesis of cryptophycins has been developed in which (5S,6R)-5-hydroxy-6-methyl-8-phenylocta-2(E),7(E)-dienoic acid (A) is coupled with an amino acid segment (B). Two stereo-selective routes to A are described, the first employing allylation of an alpha-homochiral aldehyde and the second using asymmetric crotylation of an achiral aldehyde to establish the two stereogenic centers present in A. The styryl moiety of A was attached either via Stille coupling or through a Wadsworth-Emmons condensation with diethyl benzylphosphonate. The amino acid subunit B was prepared from benzyl (2S)-2-hydroxyisocaproate by connection first to AT-Boc-beta-alanine or its (2R)-methyl-substituted derivative and then to (2R)-N-Boc-O-methyltyrosine or its m-chloro derivative. Fusion of the A and B subunits was accomplished by initial esterification of the former with the latter, followed by macrocyclization using diphenyl phosphorazidate. In this way, cryptophycin-3, -4, and -29 were obtained along with the nonnatural cyclic depsipeptide 52. Epoxidation of cryptophycin-3 with dimethyldioxirane gave cryptophycin-1; analogous epoxidation of 52 afforded arenastatin A (cryptophycin-24).

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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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Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties

The melanocortin-1 receptor (MC-1R) is a G-protein-coupled receptor involved in inflammation and skin pigmentation. Compound 2 is the first highly potent and selective MC-1R small-molecule agonist reported. Compound 2 showed efficacy in an acute model of inflammation, which has demonstrated the role of MC-1R in modulation of inflammation.

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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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Discovery of pyrrolopyrimidine inhibitors of Akt

The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knockdown of phospho-PRAS40 levels in LNCaP cells and tumor xenografts.

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

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119139-23-0, Name is 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, belongs to chiral-nitrogen-ligands compound, is a common compound. 119139-23-0In an article, authors is Arbuckle, William, once mentioned the new application about 119139-23-0.

Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist

The previously described lead compound 5 is a potent and selective V 1A antagonist with affinity at both the rat and human receptor, but displays poor oral bioavailability and moderate clearance. We report herein the successful optimisation of the pharmacokinetic (PK) properties to afford the potent, selective, orally bioavailable and CNS penetrant compound 15f. A custom optimisation approach was required which demonstrated the value of using early, rapid in vivo PK studies to show improvements in oral exposure. Such assays may be of particular value where low oral bioavailability is anticipated to be multifactorial (e.g., permeability, gut wall metabolism and/or transport) where satisfactory modelling of in vitro data is likely to be difficult within a drug discovery context.

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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 119139-23-0

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, 119139-23-0, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 119139-23-0, Name is 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, molecular formula is C20H13N3O2. In a Article, authors is Rej, Rabindra£¬once mentioned of 119139-23-0

Total synthesis of cryptophycins and their 16-(3-phenylacryloyl) derivatives

Cryptophycin A, a cyclic depsipeptide isolated from the blue-green alga (cyanobacterium) Nostoc sp.GSV 224, has shown excellent activity against solid tumors implanted in mice. The benzylic epoxide, which was shown to be very important for biological activity, is also fairly unstable under both acidic and alkaline conditions. The high doses needed to observe in vivo activity might be a result of this instability. In order to solve this problem while preserving the electrophilic character of the benzylic position, enones 1 and 2 have been proposed as promising analogs of the natural product, and a convergent total synthesis of these compounds is described. In addition, the same strategy was used to prepare Cryptophycins A,B, C, and D.

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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

The effect of the change of 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione synthetic route on the product

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One of the major reasons is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level.119139-23-0, 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, introduce a new downstream synthesis route. 119139-23-0

EXAMPLE 13 20 ml of a 1M solution of LiAlH4 in diethyl ether was added to a solution of 1.0 g of 3,4-bis(3-indolyl)-1H-pyrrole-2,5-dione in 140 ml of THF. The mixture was stirred for 18 hours under nitrogen. The mixture was cooled to 0 C., quenched with 50 ml of water, then acidified to pH 2 with 2M hydrochloric acid and extracted with ethyl acetate. The organic extracts were washed with saturated sodium bicarbonate solution, dried and evaporated. The residue was purified on silica gel with 5-10% methanol in dichloromethane. The first product eluted was triturated with ethyl acetate/hexane to give 175 mg of 3,4-bis(3-indolyl)-3-pyrrolin-2-one, m.p. 290-293 C. (decomposition). The second product eluted was crystallized from ethyl acetate/chloroform to give 490 mg of 5-hydroxy-3,4-bis(3-indolyl)-3-pyrrolin-2-one, m.p. above 250 C. (decomposition).

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Reference£º
Patent; Hoffmann-La Roche Inc.; US5057614; (1991); A;,
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

Flexible application of 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione in synthetic route

119139-23-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,119139-23-0 ,3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, other downstream synthetic routes, hurry up and to see

119139-23-0, Rate laws may be derived directly from the chemical equations for elementary reactions. This is not the case, however, for ordinary chemical reactions.119139-23-0, name is 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, below Introduce a new synthetic route.

EXAMPLE 14 820 mg of Lawesson’s reagent was added to a solution of 330 mg of 3,4-bis(3-indolyl)-1H-pyrrole-2,5-dione in 50 ml of dimethoxyethane and the mixture was heated to reflux for 1 hour. 410 mg of Lawesson’s reagent were then added and the mixture was heated to reflux for a further 1 hour. The solvent was evaporated and the residue was purified on silica gel with ethyl acetate/hexane (1:4). Recrystallization from diethyl ether/hexane gave 30 mg of 5-thioxo-3,4-bis(3-indolyl)-3-pyrrolin-2-one, m.p. 254-257 C.

119139-23-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,119139-23-0 ,3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Hoffmann-La Roche Inc.; US5057614; (1991); A;,
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

Flexible application of 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione in synthetic route

There are, however, a few established termolecular elementary reactions. The reaction of nitric oxide with oxygen appears to involve termolecular steps. you can also browse my other articles about 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, CAS: 119139-23-0

The molecularity of an elementary reaction is the number of molecules that collide during that step in the mechanism. If there is only a single reactant molecule in an elementary reaction, that step is designated as unimolecular.119139-23-0, name is 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione. A new synthetic method of this compound is introduced below. , 119139-23-0

General procedure: A reaction flask equipped with a magnetic stirrer was charged with a solution of 3, 4-bisindolylmaleimide (2.1 g, 6.4 mmol) in 100 mL of acetone. Potassium hydroxide (0.40 g, 7.1 mmol) was added to the solution at 0 C and stirred for 0.5 h. Iodomethane (1.6 g, 0.011 mol) or 1-bromooctane (2.4 g, 0.012 mol) was added to the reaction mixture for 3, 4-bisindolyl-1-N-methylmaleimide or 3, 4-bisindolyl-1-N-(n-octyl)maleimide, respectively. The reaction mixture was warmed to room temperature and stirred for 1 h (iodomethane) or 24 h (1-bromooctane). The reaction mixture was concentrated and then dissolved in a mixture of ethyl acetate and water. The organic phase was separated, washed with water once and brine once, dried over anhydrous sodium sulfate. The product was purified by flash chromatography with petroleum ether, ethyl acetate and dichloromethane (V/V = 3:1:2) as eluent.

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Reference£º
Article; Zhang, Qianfeng; Chang, Guanjun; Zhang, Lin; Chinese Chemical Letters; vol. 29; 3; (2018); p. 513 – 516;,
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