Top Picks: new discover of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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NOVEL BRONCHODILATING ISOQUINOLINE CARBAMATES

The invention relates to novel compounds having the general formula (I), and which molecules are useful to manufacture a medicament to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma, and vasoconstriction, e.g. hypertension.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of 214894-89-0

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A practical olefin hydroboration under liquid-liquid phase transfer catalysis conditions

The hydroboration of a series of representative olefins under LL-PTC conditions, followed by oxidative workup provides the corresponding alcohols in excellent yields and regio- and stereoselectivity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Brief introduction of Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate

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Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups

Tetrahydrobenzodifuran functionalities were employed as conformationally restricted bioisosteres of the aromatic methoxy groups in prototypical hallucinogenic phenylalkylamines 1 and 2. Thus, a series of 8-substituted 1- (2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b’]difuran-4-yl)-2-aminoalkanes (7a-e) were prepared and evaluated for activity in the two-lever drug discrimination paradigm in rats trained to discriminate saline from LSD tartrate (0.08 mg/kg) and for the ability to displace [3H]ketanserin from rat cortical homogenate 5-HT(2A) receptors and [3H]-8-OH-DPAT from rat hippocampal homogenate 5-HT(1A) receptors. In addition, 1-(8-bromo-2,3,6,7- tetrahydrobenzo[1,2-b:4,5-b’]difuran-4-yl)-2-aminopropane (7b), which was found to be extremely potent in the rat in vivo assays, was evaluated for its ability to compete with [125I]DOI and [3H]ketanserin binding to cells expressing cloned human 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptors. All of the dihydrofuranyl compounds having a hydrophobic substituent para to the alkylamine side chain had activities in both the in vitro and in vivo assays that equaled or surpassed the activity of the analogous conformationally flexible parent compounds. For example, 7b substituted for LSD in the drug discrimination assay with an ED50 of 61 nmol/kg and had K(i) values in the nanomolar to subnanomolar range for the displacement of radioligand from rat and human 5-HT2 receptors, making it one of the most potent hallucinogen- like phenylalkylamine derivatives reported to date. The results suggest that the dihydrofuran rings in these new analogues effectively model the active binding conformations of the methoxy groups of the parent compounds 1 and 2. In addition, the results provide information about the topography and relative orientation of residues involved in agonist binding in the serotonin 5-HT2 receptors.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthetic Route of 214894-89-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, molecular formula is C9H9BrO2. In a Patent£¬once mentioned of 214894-89-0

BICYCLIC PYRIMIDONE COMPOUNDS

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

Can You Really Do Chemisty Experiments About 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists

The design, synthesis and structure-activity relationships of a novel class of N-phenylpyridone MCH1R antagonists are described. The core part of the N-phenylpyridone structure was newly designed and the side chain moieties that were attached to the core part were extensively explored. As a result of optimization of the N-phenylpyridone leads, we successfully developed the orally available, and brain-penetrable MCH1R selective antagonist 7c, exhibiting excellent anti-obese effect in diet-induced obese (DIO) mice.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Hydrogenation of Esters to Alcohols Catalyzed by Defined Manganese Pincer Complexes

The first manganese-catalyzed hydrogenation of esters to alcohols has been developed. The combination of Mn(CO)5Br with [HN(CH2CH2P(Et)2)2] leads to a mixture of cationic and neutral Mn PNP pincer complexes, which enable the reduction of various ester substrates, including aromatic and aliphatic esters as well as diesters and lactones. Notably, related pincer complexes with isopropyl or cyclohexyl substituents showed very low activity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Properties and Exciting Facts About 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Design, synthesis and pharmacological activity of novel enantiomerically pure phosphonic acid-based NAALADase inhibitors

Inhibitors of NAALADase have shown promise for a variety of diseases associated with glutamate excitotoxicity, and could be useful for the diagnosis and therapy of prostate cancer. A series of novel enantiomerically pure 2-(phosphonomethyl)pentanedioic acid (2-PMPA) based NAALADase inhibitors were synthesized. These compounds were prepared from previously reported (S)-2-(hydroxyphosphinoylmethyl)pentanedioic acid benzyl ester 4. Biological test results showed that the new compounds are good to outstanding NAALADase inhibitors. Compounds 8b and 10b showed activity similar to the known potent inhibitor (S)-2-PMPA. Fluorescently labeled inhibitor 19b may potentially be used to study binding to prostate cancer cells by fluorescence microscopy, and siderophore-containing inhibitor 21b may be useful for detection of prostate-derived cancer cells by magnetic resonance imaging (MRI). This journal is The Royal Society of Chemistry.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists

Herein, we report the synthesis and structure?activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D4) antagonists. A series of compounds from this scaffold are highly potent against the D4receptor and selective against the other dopamine receptors. In addition, we were able to confirm the active isomer as the (R)-enantiomer via an X-ray crystal structure.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists

Compounds represented by Formula (I): 1or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem