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beta-Phenylethylidenehydrazine (PEH) has been demonstrated previously to be an inhibitor of gamma-aminobutyric acid transaminase (GABA-T) and to cause a marked increase in rat brain levels of GABA, a major neurotransmitter. A group of PEH analogs, possessing a variety of substituents (Me, OMe, Cl, F, and CF3) at the 2-, 3-, and 4-positions of the phenyl ring, were synthesized for evaluation as inhibitors of GABA-T. The details of the synthesis and chemical characterization of the analogs are described. Preliminary in vitro screening for GABA-T inhibition showed that all the analogs possessed activity against this enzyme, although substitution of CF3 at the 2- and 4-positions caused reduced activity. One of the drugs, 4-fluoro-beta- phenylethylidenehydrazine, was investigated further ex vivo, where it was shown to inhibit GABA-T, elevate brain levels of GABA, and decrease levels of glutamine, similar to the profile observed previously for PEH.

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

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The BH4– promoted electrochemical hydrodefluorination of fluoroaromatic compounds was reported. Using platinum as electrodes in an undivided cell, the electrolysis was carried out at constant current at room temperature under air without the need of pretreatment of the solvent. This reaction could proceed smoothly on both nonactivated monofluoroarenes and perfluoroarenes with high yields and good selectivities.

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

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The transformation of simple hydrocarbons into more complex and valuable products has revolutionised modern synthetic chemistry. This type of reactivity has quickly become one of the cornerstones of modern catalysis.Recommanded Product: 214894-89-0, In a article, mentioned the application of 214894-89-0, molecular formula is C9H9BrO2

Ring the changes: The direct cross-coupling of electron-deficient 1,4-benzoquinone or its derivatives with electron-rich alkyl vinyl ethers proceeds in a tandem manner to produce substituted benzene rings with good selectivity and in good to excellent yields (see scheme). The reaction has the potential for the rapid synthesis of diverse substituted benzene rings as it is not limited by substituent effects. Copyright

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

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This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: Z represents a hydrogen atom or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Related Products of 214894-89-0, In homogeneous catalysis, catalysts are in the same phase as the reactants. Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. In a document type is Patent, and a compound is mentioned, CAS :214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, introducing its new discovery.

The present invention relates to novel bicyclic pyrimidone compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer’s disease.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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hemistry is a science major with cience and engineering. The main research directions are chemical synthesis, preparation and modification of special coatings, and research on the structure and performance of functional materials , Quality Control of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine. Introducing a new discovery about 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

Alcohol synthesis is critical to the chemical and pharmaceutical industries. The addition of water across olefins to form primary alcohols (anti-Markovnikov olefin hydration) would be a broadly useful reaction but has largely proven elusive; an indirect hydroboration/oxidation sequence requiring stoichiometric borane and oxidant is currently the most practical methodology. Here, we report a more direct approach with the use of a triple relay catalysis system that couples palladium-catalyzed oxidation, acid-catalyzed hydrolysis, and ruthenium-catalyzed reduction cycles. Aryl-substituted terminal olefins are converted to primary alcohols by net reaction with water in good yield and excellent regioselectivity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2?-position of phenylethanol moiety could significantly enhance CAPE’s antiproliferative activity. 2?-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50?=?0.4?¡À?0.02 & 0.6?¡À?0.03?muM against Hela and DU-145 respectively).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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In this paper we describe the synthesis of a series of alpha-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR) agonist (1S,1’S,2’S)-carboxycyclopropylglycine (2, L-CCG 1). Incorporation of a substituent on the amino acid carbon converted the agonist 2 into an antagonist. All of the compounds were prepared and tested as a series of four isomers, i.e., two racemic diastereomers. On the basis of the improvement in affinity realized for the alpha-phenylethyl analogue 3, in this paper we explored the effects of substitution on the aromatic ring as a strategy to increase the affinity of these compounds for group II mGluRs. Affinity for group II mGluRs was measured using [3H]glutamic acid (Glu) binding in rat forebrain membranes. Antagonist activity was confirmed for these compounds by measuring their ability to antagonize (1S,3R)-1- aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells transfected with human mGluR2 and mGluR3. Meta substitution on the aromatic ring of 3 with a variety of substituents, both electron donating (e.g., methyl, hydroxy, amino, methoxy, phenyl, phenoxy) and electron withdrawing (e.g., fluorine, chlorine, bromine, carboxy, trifluoromethyl) gave from 1.5- to 4.5-fold increases in affinity. Substitution with p-fluorine, as in 97 (IC50 = 0.022 ¡À 0.002), was the exception. Here, a greater increase in affinity was realized than for either the ortho- or meta-substituted analogues; 97 was the most potent compound resulting from monosubstitution of the aromatic. At best, only modest increases in affinity were realized for certain compounds bearing either two chlorines or two fluorines, and two methoxy groups gave no improvement in affinity (all examined in a variety of substitution patterns). Three amino acids, 4, 5, and 104, were resolved into their four constituent isomers, and affinity and functional activity for group II mGluRs was found to reside solely in the S,S,S-isomers of each, consistent with 1. With an IC50 = 2.9 ¡À 0.6 nM, the resolved xanthylmethyl compound 168 was the most potent compound from this SAR. Amino acid 168 demonstrated high plasma levels following intraperitoneal (ip) administration and readily penetrated into the brain. This compound, however, had only limited (~5%) oral bioavailability. Systemic administration of 168 protected mice from limbic seizures produced by the mGluR agonist 3,5-dihydroxyphenylglycine, with an ED50 = 31 mg/kg (ip, 60 min preinjection). Thus, 168 represents a valuable tool to study the role of group II mGluRs in disease.

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

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Photochemical Transformation of O-(beta-Arylethyl) Arylimidates into 2,4-Diaryl-5-iodoxazoles with 1,3-Diiodo-5,5-dimethylhydantoin

Treatment of O-(beta-arylethyl) arylimidates with 1,3-diiodo-5,5-dimethylhydantoin (DIH) under irradiation with a tungsten lamp in 1,2-dichloroethane gave the corresponding 2,4-diaryl-5-iodoxazoles and 2,4-diaryloxazoles in good to moderate yields, respectively, depending on the aryl group. It was proposed that the reactions proceeded through the formation of N-iodoimidates by the reaction of O-(beta-arylethyl) arylimidates with DIH, followed by the formation of iminyl radicals via homolytic N?I bond cleavage, the 1,5-H shift by the iminyl radicals, the C?I bond formation of the formed carbon-centered radicals with iodine, the nucleophilic cyclization by the imino groups to form 2,4-diaryloxazolines, the oxidation of the formed 2,4-diaryloxazolines to 2,4-diaryloxazoles, and the iodination of the formed 2,4-diaryloxazoles to 2,4-diaryl-5-iodoxazoles with DIH.

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