Category: 652-39-1

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The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

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Reference：
Benzofuran – Wikipedia,
Benzofuran | C8H2471O – PubChem

Can You Really Do Chemisty Experiments About 4-Fluoroisobenzofuran-1,3-dione

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 652-39-1 is helpful to your research. Application of 652-39-1

Application of 652-39-1, 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, 652-39-1, molcular formula is C8H3FO3, introducing its new discovery.

Differently substituted phthalic anhydrides can react either with semicarbazide or thiosemicarbazide to give respectively 1,4-dioxo-3,4-dihydrophthalazine-2(1H)-carboxamides or 1,4-dioxo-3,4-dihydrophthalazine-2(1H)-carbothioamides under mild conditions and generally with good yields. These compounds have been tested in order to evaluate their anti-microbial activity. Furthermore a new synthetic pathway to phtha-lazino[2,3-b]phthalazine-5,7,12,14-tetraone has been devised.

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Reference：
Benzofuran – Wikipedia,
Benzofuran | C8H2514O – PubChem

Awesome and Easy Science Experiments about 4-Fluoroisobenzofuran-1,3-dione

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Metal hydride reductions of planar cyclic anhydrides such as methylmaleic or 3-substituted phthalic anhydrides occur preferentially at the sterically more hindered carbonyl function.This regioselectivity cannot be rationalized in terms of “the most favourable pathway for non-perpendicular attack by a nucleophile” since both carbonyl groups present are equally accessible to non-perpendicular approach.A study which takes into account the alkaline cation and inductive, mesomeric, and steric effects has been conducted for the reduction of several conjugated and aromatic anhydrides.A qualitative interpretation for the regioselectivities observed in these reductions (as well as in reductions already reported in the literature) is suggested.An early transition state for the catalyzed versus late transition state for the non-catalyzed process is proposed.

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Reference：
Benzofuran – Wikipedia,
Benzofuran | C8H2532O – PubChem

More research is needed about 652-39-1

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Different 1,4-dioxo-3,4-dihydrophthalazine-2(1H)-carboxamide and -carbothioamide derivatives were synthesized in a simple and environmentally benign method from the reaction of different phthalic anhydrides with semicarbazide or thiosemicarbazide using montmorillonite KSF clay as solid acidic catalyst and microwave irradiations under the solvent-free conditions in good yields and short reaction times.

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Reference：
Benzofuran – Wikipedia,
Benzofuran | C8H2529O – PubChem

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To obtain selective and potent inhibitors of dipeptidyl peptidases 8 and 9, we synthesized a series of substituted isoindolines as modified analogs of allo-Ile-isoindoline, the reference DPP8/9 inhibitor. The influence of phenyl substituents and different P2 residues on the inhibitors’ affinity toward other DPPs and more specifically, their potential to discriminate between DPP8 and DPP9 will be discussed. Within this series compound 8j was shown to be a potent and selective inhibitor of DPP8/9 with low activity toward DPP II.

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Reference：
Benzofuran – Wikipedia,
Benzofuran | C8H2560O – PubChem

Discovery of 4-Fluoroisobenzofuran-1,3-dione

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Nickel-catalyzed decarbonylative cycloaddition of phthalic anhydrides with 1,3-Dienes

An intermolecular nickel-catalyzed decarbonylative [4 + 2] cycloaddition has been developed where phthalic anhydrides react with 1,3-dienes to afford substituted 3-vinyldihydroisocoumarins.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2521O – PubChem

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CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS

The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2497O – PubChem

Can You Really Do Chemisty Experiments About 4-Fluoroisobenzofuran-1,3-dione

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Novel phthalamides containing sulfiliminyl moieties and derivatives as potential ryanodine receptor modulators

To tackle the serious challenge of insect resistance and stricter environmental regulations, innovating a new eco-friendly insecticide is urgently required. A series of new phthalamides containing sulfiliminyl and sulfoximinyl moieties were designed and synthesized. In total, 30 new structures were characterized by 1H NMR spectra and HRMS. The bioassay results indicated that some title compounds exhibited excellent insecticidal activities against oriental armyworm (Pseudaletia separata Walker) and diamondback moth (Plutella xylostella (L.)). 4a showed the same larvicidal level as that of commercial flubendiamide as a control. 7a and 9a exhibited outstanding activity against diamondback moth. The LC50 values of 7a and 9a were 8.33 ¡Á 10-8 and 2.34 ¡Á 10-8 mg L-1, respectively, lower than that of flubendiamide (1.25 ¡Á 10-7 mg L-1). The effects of 4a, 7a and 9a on intracellular calcium of neurons from the beet armyworm (Spodoptera exigua) indicated that these title compounds activate the receptor-operated calcium channel. The calcium ions efflux from the calcium store on endoplasmic reticulum (ER) when treated with novel compounds. The results of CoMFA calculation showed that N-cyanosulfilimines and N-trifluoroacetylsulfoximines might be of importance to the larvicidal activity. The present work demonstrated that structures containing sulfiliminyl and sulfoximinyl moieties can be considered as lead compounds for the development of new insect ryanodine receptor modulators. This journal is the Partner Organisations 2014.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2570O – PubChem

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Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for metabotropic glutamate receptor subtype 4 (mGlu4)

Four 4-phthalimide derivatives of N-(3-chlorophenyl)-2-picolinamide were synthesized as potential ligands for the PET imaging of mGlu4 in the brain. Of these compounds, N-(3-chloro-4-(4-fluoro-1,3-dioxoisoindolin-2-yl)phenyl)-2-picolinamide (3, KALB001) exhibited improved binding affinity (IC50 = 5.1 nM) compared with ML128 (1) and was subsequently labeled with 18F. When finally formulated in 0.1 M citrate buffer (pH 4) with 10% ethanol, the specific activity of [18F]3 at the end of synthesis (EOS) was 233.5 ¡À 177.8 GBq/mumol (n = 4). The radiochemical yield of [18F]3 was 16.4 ¡À 4.8% (n = 4), and the purity was over 98%. In vivo imaging studies in a monkey showed that the radiotracer quickly penetrated the brain with the highest accumulation in the brain areas known to express mGlu4. Despite some unfavorable radiotracer properties like fast washout in rodent studies, [18F]3 is the first 18F-labeled mGlu4 radioligand, which can be further modified to improve pharmacokinetics and brain penetrability for future human studies.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2533O – PubChem

The important role of 4-Fluoroisobenzofuran-1,3-dione

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HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN DEGRADATION

This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2493O – PubChem