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N-Aryloxylethylindolealkylamines (5) having dual 5-HT transporter and 5-HT1A affinity are described. These compounds represent truncated analogues of our previously reported piperidinyl derivatives (3). Compounds in this investigation were found to have more similar affinities and functional activities for the 5-HT1A receptor and 5-HT transporter. Though 5-HT1A antagonism is not consistently observed throughout series 5, several molecular features were found to be essential to obtain high and balanced activities. The proper placement of a heteroatom in the aryl ring and the length of the linkage used to tether the indole moiety had significant influence on 5-HT1A and 5-HT transporter affinities. Introduction of a halogen into the aryl ring usually lowered intrinsic activity and in some cases led to full 5-HT1A antagonists. Compounds 33 and 34 were observed to be full 5-HT1A antagonists with Ki values of approximately 30 nM for the 5-HT1A receptor and Ki values of 5 and 0.5 nM for the 5-HT transporter, respectively. Unfortunately, similar to our previous series (3), compounds in this report also had high affinity for the alpha1 receptor.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H564O – PubChem

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Visible light-induced monofluoromethylenation of benzofurans and benzothiophenes with ethyl bromofluoroacetate was developed. This method provided a convenient access to novel alpha-fluoro-alpha-heteroarylesters under mild reaction conditions.

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Benzofuran – Wikipedia,
Benzofuran | C8H572O – PubChem

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24410-59-1, Name is 5-Fluorobenzofuran, belongs to benzofurans compound, is a common compound. Computed Properties of C8H5FOIn an article, once mentioned the new application about 24410-59-1.

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 is a C6-C14 aromatic cyclic hydrocarbon group etc.; R2, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C1-C6 alkylene group etc.; X is a single bond, or a group represented by -CO-NH- or -NH-CO-, etc.; and Y is a C3-C8 cycloalkyl group, a C6-C14 aromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

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Reference:
Benzofuran – Wikipedia,
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A Pd-catalyzed, asymmetric oxidative cross-coupling reaction between ferrocenes and heteroarenes is described. The process, which takes place via a twofold C-H bond activation pathway, proceeds with modest to high efficiencies (36-86%) and high levels of regio- and enantioselectivity (95-99% ee). In the reaction, air oxygen serves as a green oxidant and excess amounts of the coupling partners are not required. The process is the first example of a catalytic asymmetric biaryl coupling reaction that occurs via double C-H bond activation. Finally, the generated coupling products can be readily transformed into chiral ligands and catalysts.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H561O – PubChem

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 24410-59-1, name is 5-Fluorobenzofuran, introducing its new discovery. Formula: C8H5FO

The first example of sole direct C-H bond arylation of benzo[b]furans with aryl chlorides was achieved catalyzed by a well-defined NHC-Pd(II)-Im complex. Under the suitable conditions, all reactions involving kinds of benzo[b]furans and (hetero)aryl chlorides proceeded well to give the desired C2-arylated benzo[b]furans in sole regioselectivity in acceptable to high yields, providing an efficient and economic pathway for the direct C2-H bond arylation of benzo[b]furans.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H571O – PubChem

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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H556O – PubChem

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Electric Literature of 24410-59-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.24410-59-1, Name is 5-Fluorobenzofuran, molecular formula is C8H5FO. In a Patent,once mentioned of 24410-59-1

Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H556O – PubChem

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Palladium-catalyzed regioselective cross-dehydrogenative coupling of benzofurans with uracils at room temperature

The Pd-catalyzed cross-dehydrogenative coupling (CDC) between two heteroarenes was developed. A variety of benzofuran and uracil derivatives were constructed through C-C bond formation by using CDC reactions. The substrates did not require prefunctionalization, and the products were obtained in good yields with good regioselectivities at room temperature. The Pd-catalyzed cross-dehydrogenative coupling (CDC) between two heteroarenes is developed. A variety of benzofuran and uracil derivatives are constructed in good yields with good regioselectivity at room temperature through C-C bond formation by using CDC reactions; prefunctionalization of the substrates is not required. PivOH = pivalic acid.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H562O – PubChem

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Related Products of 24410-59-1, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 24410-59-1, 5-Fluorobenzofuran, introducing its new discovery.

Biocatalytic Strategy for Highly Diastereo- and Enantioselective Synthesis of 2,3-Dihydrobenzofuran-Based Tricyclic Scaffolds

2,3-Dihydrobenzofurans are key pharmacophores in many natural and synthetic bioactive molecules. A biocatalytic strategy is reported here for the highly diastereo- and enantioselective construction of stereochemically rich 2,3-dihydrobenzofurans in high enantiopurity (>99.9% de and ee), high yields, and on a preparative scale via benzofuran cyclopropanation with engineered myoglobins. Computational and structure-reactivity studies provide insights into the mechanism of this reaction, enabling the elaboration of a stereochemical model that can rationalize the high stereoselectivity of the biocatalyst. This information was leveraged to implement a highly stereoselective route to a drug molecule and a tricyclic scaffold featuring five stereogenic centers via a single-enzyme transformation. This work expands the biocatalytic toolbox for asymmetric C?C bond transformations and should prove useful for further development of metalloprotein catalysts for abiotic carbene transfer reactions.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H569O – PubChem

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Derisking the Cu-Mediated 18F-Fluorination of Heterocyclic Positron Emission Tomography Radioligands

Molecules labeled with fluorine-18 (18F) are used in positron emission tomography to visualize, characterize and measure biological processes in the body. Despite recent advances in the incorporation of 18F onto arenes, the development of general and efficient approaches to label radioligands necessary for drug discovery programs remains a significant task. This full account describes a derisking approach toward the radiosynthesis of heterocyclic positron emission tomography (PET) radioligands using the copper-mediated 18F-fluorination of aryl boron reagents with 18F-fluoride as a model reaction. This approach is based on a study examining how the presence of heterocycles commonly used in drug development affects the efficiency of 18F-fluorination for a representative aryl boron reagent, and on the labeling of more than 50 (hetero)aryl boronic esters. This set of data allows for the application of this derisking strategy to the successful radiosynthesis of seven structurally complex pharmaceutically relevant heterocycle-containing molecules.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H568O – PubChem