Day: June 8, 2021

Electric Literature of 2879-20-1, New Advances in Chemical Research, May 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. In a document type is Article, and a compound is mentioned, 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, introducing its new discovery.

A method for the synthesis of diversely substituted 3-fluoropyridines from two ketone components is described. The reaction involves photoredox coupling of alpha,alpha-difluoro-beta-iodoketones with silyl enol ethers catalyzed by fac-Ir(ppy)3 under blue LED irradiation with subsequent one-pot condensation with ammonium acetate. Based on cyclic voltammetry studies, it was determined that alpha,alpha-difluoro-beta-iodoketones are reduced notably easier compared to 2,2,2-trifluoro-1-iodoethane, which may be ascribed to the influence of the carbonyl group.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New discoveries in chemical research and development in 2021. Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage. In a patent，Which mentioned a new discovery about Formula: C9H9BrO2, Formula: C9H9BrO2

The conversion of terminal alkynes to functionalized products by the direct addition of heteroatom-based nucleophiles is an important aim in catalysis. We report the design, synthesis, and mechanistic studies of the half-sandwich ruthenium complex 12, which is a highly active catalyst for the anti-Markovnikov reductive hydration of alkynes. The key design element of 12 involves a tridentate nitrogen-based ligand that contains a hemilabile 3-(dimethylamino) propyl substituent. Under neutral conditions, the dimethylamino substituent coordinates to the ruthenium center to generate an air-stable, 18-electron, kappa3-complex. Mechanistic studies show that the dimethylamino substituent is partially dissociated from the ruthenium center (by protonation) in the reaction media, thereby generating a vacant coordination site for catalysis. These studies also show that this substituent increases hydrogenation activity by promoting activation of the reductant. At least three catalytic cycles, involving the decarboxylation of formic acid, hydration of the alkyne, and hydrogenation of the intermediate aldehyde, operate concurrently in reactions mediated by 12. A wide array of terminal alkynes are efficiently processed to linear alcohols using as little as 2 mol % of 12 at ambient temperature, and the complex 12 is stable for at least two weeks under air. The studies outlined herein establish 12 as the most active and practical catalyst for anti-Markovnikov reductive hydration discovered to date, define the structural parameters of 12 underlying its activity and stability, and delineate design strategies for synthesis of other multifunctional catalysts.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. Recommanded Product: 3663-79-4, In a article, mentioned the application of 3663-79-4, Name is Methyl 1,4-Benzodioxane-2-carboxylate, molecular formula is C10H10O4

A series of 2,3-dihydrobenzo[b][1,4]dioxin- and indolealkylamine derivatives were synthesized and the target compounds were evaluated for their binding affinities at the 5-HT1A receptor and serotonin transporter. Antidepressant-like activities of the compounds were screened using the tail suspension and forced swim tests in mice. Preliminary results indicated that the target compounds exhibited high binding affinities at the 5-HT1A receptor and serotonin transporter, and produced marked antidepressant-like effects. The best example from this study, compound 5, exhibited high binding affinities for the 5-HT1A receptor (Ki = 96 nM) and serotonin transporter (Ki = 9.8 nM). The intrinsic activity of compound 5 showed agonistic property to the 5-HT1A receptor and inhibition of the 5-HT transporter. Furthermore, compound 5 exhibited greater antidepressant efficacy than fluoxetine and showed acceptable pharmacokinetic properties. A series of 3-(2-(4-((2,3-dihydrobenzo[b][1,4]dioxin-3-yl)methyl) piperazin-1-yl)ethyl-1H-indole derivatives were synthesized and the target compounds were evaluated for their antidepressant activities in vitro and in vivo. The compounds described were also evaluated for dual 5-HTT and 5-HT 1A receptor activities.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Related Products of 214894-89-0, New Advances in Chemical Research, May 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. In a document type is Patent, and a compound is mentioned, 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, introducing its new discovery.

The present invention provides various processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme: 1

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Research speed reading in 2021.The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. COA of Formula: C9H8O4, In a article, mentioned the application of 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4

This Letter discloses a series of 2-aminothiadiazole amides as selective EP3 receptor antagonists. SAR optimization resulted in compounds with excellent functional activity in vitro. In addition, efforts to optimize DMPK properties in the rat are discussed. These efforts have resulted in the identification of potent, selective EP3 receptor antagonists with excellent DMPK properties suitable for in vivo studies.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 4442-53-9, and how the biochemistry of the body works.COA of Formula: C9H8O4

Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Application of 2879-20-1, Research speed reading in 2021. The prevalence of solvent effects has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and their interactions with reaction intermediates. In a document type is Article, and a compound is mentioned, 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, introducing its new discovery.

Substituted 1,4-benzoxazines bearing an amino side chain at the 2- position were prepared and were found to have a moderate activity on intracellular calcium. Of the compounds studied it was found that those which possess a homoveratrylamino moiety exhibited superior potency. The chain length and the nature of the amine (4-fluorophenylpiperazine, 4- fluorobenzhydryloxyethylamine, N-substituted homoveratrylamine) is discussed. The 4-benzyl-3,4-dihydro-2-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]- 2H-1,4-benzoxazine (3c) is the most potent derivative of the series with a ratio of IC50 values against PE (phenylephrine) and K+ of 2.1. Under these test conditions a ratio near 1 indicates potential intracellular calcium activity while a ratio greater than 100 an action on extracellular calcium influx.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Synthetic Route of 2879-20-1, Research speed reading in 2021. The prevalence of solvent effects has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and their interactions with reaction intermediates. In a document type is Article, and a compound is mentioned, 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, introducing its new discovery.

A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure?activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New research progress on 10288-72-9 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. Formula: C8H8O3, In a article, mentioned the application of 10288-72-9, Name is 6-Hydroxy-1,4-benzodioxane, molecular formula is C8H8O3

An efficient and highly regioselective iron(III)-catalyzed Friedel?Crafts-type arylation of spiro-epoxyoxindoles with phenols was developed for rapid access to 3-(3-indolyl)-oxindole-3-methanols, which could be further elaborated into benzofuranyl-spirooxindoles under Mitsunobu conditions. When spiro-epoxyoxindoles were reacted with naphthols in the presence of a catalytic amount of FeCl3?6 H2O in dichloromethane, they underwent a tandem Friedel?Crafts-type arylation and O-cyclization to yield novel naphthofuranyl-spirooxindoles in excellent yields. This method is applied to enable the efficient and highly regioselective synthesis of a small-molecule inhibitor of the sodium channel Nav1.7 (±)-XEN402, which is currently in a phase IIb clinical trial for the treatment of pain.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. category: benzodioxans, In a article, mentioned the application of 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, molecular formula is C9H9BrO2

With the aim to discover a gastric antisecretory agent more potent than the existing proton pump inhibitors, novel 3,4-dihydro-1H-spiro(naphthalene-2,2?-piperidin)-1-one derivatives, which could occupy two important lipophilic pockets (described as LP-1 and LP-2) of H+,K+-ATPase and can strongly bind to the K+-binding site, were designed based on a docking model. Among the compounds synthesized, compound 4d showed a strong H+,K+-ATPase-inhibitory activity and a high stomach concentration in rats, resulting in potent inhibitory action on histamine-stimulated gastric acid secretion in rats. Furthermore, 4d exerted significant inhibitory action on histamine-stimulated gastric-acid secretion in rats with a rapid onset and moderate duration of action after the administration. These findings may lead to a new insight into the drug design of potassium-competitive acid blockers.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. category: benzodioxans, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 214894-89-0, in my other articles.

Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New discoveries in chemical research and development in 2021. Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage. In a patent，Which mentioned a new discovery about Recommanded Product: 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, Recommanded Product: 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

The air- and water-stable pi-allyliridium C,O-benzoate modified by (S)-tol-BINAP, (S)-Ir-II, catalyzes highly regio- and enantioselective Tsuji-Trost-type aminations of racemic branched alkyl-substituted allylic acetates using primary or secondary (hetero)aromatic amines. Specifically, in the presence of (S)-Ir-II (5 mol%) in DME solvent at 60-70 C, alpha-methyl allyl acetate 1a (100 mol%) reacts with primary (hetero)aromatic amines 2a-2l (200 mol%) or secondary (hetero)aromatic amines 3a-3l (200 mol%) to form the branched products of allylic amination 4a-4l and 5a-5l, respectively, as single regioisomers in good to excellent yield with uniformly high levels of enantioselectivity. As illustrated by the conversion of heteroaromatic amine 3m to adducts 6a-6g, excellent levels of regio- and enantioselectivity are retained across diverse branched allylic acetates bearing normal alkyl or secondary alkyl substituents. For reactants 3n-3p, which incorporate both primary and secondary aryl amine moieties, regio- and enantioselective amination occurs with complete site-selectivity to furnish adducts 7a-7c. Mechanistic studies involving amination of the enantiomerically enriched, deuterium-labeled acetate 1h corroborate C-N bond formation via outer-sphere addition.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem