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Pd/Cu-catalyzed dual C-H bond carbonylation towards the synthesis of fluorazones

Pd/Cu catalyzed oxidative dual C-H bond activation/carbonylation still remains a great challenge due to the generation of by-products via C-C bond formation. Herein we developed a straightforward Pd/Cu-catalyzed oxidative dual C-H bond carbonylation process to access biologically and pharmaceutically important fluorazones from easily available N-aryl pyrroles and CO. A wide range of functional groups were well tolerated in this transformation, and O2 could be utilized as the only terminal oxidant to promote the oxidative carbonylation process.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Vanilloid receptor ligands and their use in treatments

Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A combinatorial scaffold approach toward kinase-directed heterocycle libraries

A novel strategy for efficient synthesis of various substituted heterocycles as kinase-directed combinatorial libraries is described. The general scheme involves capture of various dichloroheterocycles onto solid support and further elaborations by aromatic substitution with amines at elevated temperature or by anilines, boronic acids, and phenols via palladium-catalyzed cross-coupling reactions, thus the scaffold itself is transformed into a diversity element within the combinatorial scheme. Libraries consisting of discrete and highly diverse heterocyclic small molecules constructed with these chemistries are currently being evaluated in a variety of cell and protein-based assays. Copyright

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2

Screening for Inhibitors of Acetaldehyde Dehydrogenase (AdhE) from Enterohemorrhagic Escherichia coli (EHEC)

Acetaldehyde dehydrogenase (AdhE) is a bifunctional acetaldehyde?coenzyme A (CoA) dehydrogenase and alcohol dehydrogenase involved in anaerobic metabolism in gram-negative bacteria. This enzyme was recently found to be a key regulator of the type three secretion (T3S) system in Escherichia coli. AdhE inhibitors can be used as tools to study bacterial virulence and a starting point for discovery of novel antibacterial agents. We developed a robust enzymatic assay, based on the acetaldehyde-CoA dehydrogenase activity of AdhE using both absorption and fluorescence detection models (Z? > 0.7). This assay was used to screen ~11,000 small molecules in 384-well format that resulted in three hits that were confirmed by resynthesis and validation. All three compounds are noncompetitive with respect to acetaldehyde and display a clear dose?response effect with hill slopes of 1?2. These new inhibitors will be used as chemical tools to study the interplay between metabolism and virulence and the role of AdhE in T3S regulation in gram-negative bacteria, and as starting points for the development of novel antibacterial agents.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Electric Literature of 22013-33-8, 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, 22013-33-8, molcular formula is C8H9NO2, introducing its new discovery.

Synthese et proprietes biologiques photoinduites de dioxinnocoumarines lineaires

Synthesis and photoinduced biological properties of linear dioxinocoumarins.Several dioxinocoumarins with a substituted or unsubstituted coumarin moiety were synthesized from commercially available 6-amino-1,4-benzodioxan.Qualitative assays on the photoinduced inhibition of growth in the yeast Saccharomyces cerevisiae indicate that two dioxinocoumarins are photobiologically active. The 5H-<2> benzopyrano<3,4-g><1,4>benzodioxin-5-one 1d is more active than angelicin but less active than 8-MOP.The 9-methyl-7H-pyrano<2,3-g><1,4>benzodioxin-7-one 1c is slightly less active than angelicin.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds

Three synthetic routes were developed for structure-activity relationship (SAR) studies of HTS-derived isoquinolinone inhibitor probes for the orphan nuclear receptor steroidogenic factor-1 (NR5A1). Among the new analogs reported herein, 31 and 32 have improved potency, lower cellular toxicity, and improved selectivity compared to the initial HTS-derived leads 1 and 2.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis of Symmetrical N-(Het)aryl-C-phosphonoacetamidines

A series of new symmetrical C-phosphonylated acetamidines was obtained by the reaction of diethyl chloroethynylphosphosphonate with a number of primary aromatic and heteroaromatic amines.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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LATE SV40 (LSF) INHIBITORS

The present invention is directed to compositions, methods and kits for treatment of cancer, e.g. hepatocellular carcinoma (HCC). In some embodiments, the present invention discloses the use of a small-molecule compounds of Formula (I)-(V) to inhibit tubulin methylation or to modulate chromatin or cytoskeleton modification in a cell.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthetic Route of 22013-33-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a article£¬once mentioned of 22013-33-8

Benzopyran derivatives and pharmaceutical compositions containing them

New benzopyran derivatives of formula: STR1 in which R1 is hydrogen, halogen, hydroxy, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl) amino or acylamino, X is nitrogen or a >CH-radical R is a radical of formula: STR2 in which A denotes a single bond or methylene or, when X is nitrogen, A may denote carbonyl, and R2 and R3, which are identical or different, are hydrogen, halogen, hydroxy, alkyl, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano, or, when they are adjacent, together form a methylenedioxy or ethylenedioxy radical, or else R is pyridyl or 2(2H)-benzimidazolonyl if X denotes >CH–, and R’ and R” are identical and are hydrogen or alkyl, their isomeric forms and mixtures thereof, and their acid addition salts, can be used as antiarrhythmic and antifibrillation agents.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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MULTIPLE D2 A(NTA)GONISTS/H3 ANTAGONISTS FOR TREATMENT OF CNS-RELATED DISORDERS

The present invention relates to compounds compound according to Formula (III); and pharmaceutically acceptable salts, hydrates and solvates thereof. These compounds have D2receptor antagonist/(partial) agonist effects and H3antagonistic effects, pharmaceutical compositions thereof, and methods of using them for application in the prophylaxis or treatment of CNS disorders.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem