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The Pd catalysed enantioselective hydrogenation of activated C=C bond containing compounds, unsaturated ketones, pyrones and carboxylic acids is discussed, focusing on new substrates, chiral modifiers and their mode of action.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1969O – PubChem

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A nickel-catalyzed deamidative cross-coupling reaction of amides with terminal alkynes as coupling partners was disclosed. This newly developed methodology allows the direct interconversion of amides to alkynes and enables a facile route for C(sp2)-C(sp) bond formation in a straightforward and mild fashion.

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Benzofuran – Wikipedia,
Benzofuran | C8H1975O – PubChem

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A contemporary method is reported for the Pd(OAc)2/AgOAc catalytic system based bidentate ligand directed, regioselective C-H activation and C-C bond formation at the C-3 position of thiophene- and furan-2-carboxamides, which are derived from 8-aminoquinoline or 2-(methylthio)aniline. The Pd-catalyzed C-H arylation of thiophene- and furan-2-carboxamides with a variety of aryl iodides and heteroaryl iodides was highly regioselective and afforded C-3-arylated thiophene-2-carboxamides and furan-2-carboxamides in good to very good yields. The bidentate ligand directed Pd(OAc)2/AgOAc based strategy was also successfully employed for benzylation and alkylation reactions of the thiophene-2-carboxamides. These reactions occurred with high regioselectivity to afford the C-3-benzylated and C-3-alkylated thiophene-2-carboxamides in good yields. The observed regioselectivity of these reactions was confirmed by X-ray crystal structure analyses of compounds 3e, 5a, and 6a. A contemporary method is reported for the Pd(OAc)2/AgOAc catalytic system based bidentate ligand directed, regioselective C-H activation and C-C bond formation of the C-3 position of thiophene- and furan-2-carboxamides. This protocol was used for the direct C-3 arylation and alkylation reactions of both thiophene- and furan-2-carboxamides.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1919O – PubChem

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The standard enthalpies of formation of benzofuran-, indole-, and benzothiophene-2-carboxylic acids, and 2-acetylbenzofuran in the condensed phase were measured at T = 298.15 K from experimental determinations of their energies of combustion by isoperibolic calorimetry. The enthalpies, temperatures of melting, purities and heat capacities of the compounds were determined using differential scanning calorimetry. Using thermogravimetry the enthalpies of sublimation were obtained and subsequently, the standard enthalpies of formation in the gas-phase and at T = 298.15 K for the four compounds were derived. The results of this analysis were compared with the values obtained by the Gaussian-4 procedure using the atomization method. The computational results are in good agreement with the experimental values. The influence of the heteroatom (oxygen, nitrogen and sulfur) and acetyl or carboxyl groups on the standard enthalpy of formation is also discussed.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1939O – PubChem

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The invention discloses a new class of smile lactone derivatives (formula I, II) or salt, preparation method thereof, its pharmaceutical composition and use especially in the preparation of anti-tumor and immune treatment use of the medicament. (by machine translation)

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Benzofuran – Wikipedia,
Benzofuran | C8H1681O – PubChem

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The structure-based design and synthesis of a series of novel biphenyl sulfonamide carboxylic acids as potent MMP-13 inhibitors with selectivity over MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-14, Aggrecanase 1, and TACE are described.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1876O – PubChem

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Discovery of new drug binding sites on well-established targets is of great interest as it facilitates the design of new mechanistic inhibitors to overcome the acquired drug resistance. Small chemical fragments can easily enter and bind to the cavities on the protein surface. Thus, they can be used to probe new druggable pockets in proteins. DNA gyrase plays indispensable roles in DNA replication, and both its GyrA and GyrB subunits are clinically validated antibacterial targets. New mechanistic GyrB inhibitors are urgently desired since the withdrawal of novobiocin from the market by the FDA due to its reduced efficiency and other reasons. Here, a fragment library was screened against the E. coli GyrB ATPase domain by combining affinity- and bioactivity-based approaches. The following X-ray crystallographic efforts were made to determine the cocrystal structures of GyrB with ten fragment hits, and three different binding modes were disclosed. Fortunately, a hydrophobic pocket which is previously unknown was identified by two fragments. Fragments that bind to this pocket were shown to inhibit the ATPase activity as well as the DNA topological transition activity of DNA gyrase in vitro. A set of fragment analogs were screened to explore the binding capacity of this pocket and identify the better starting fragments for lead development. Phylogenetic analysis revealed that this pocket is conserved in most Gram-negative and also many Gram-positive human pathogenic bacteria, implying a broad-spectrum antibacterial potential and a lower risk of mutation. Thus, the novel druggable pocket and the starting fragments provide a novel basis for designing new GyrB-targeting therapeutics.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1826O – PubChem

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The polymer-assisted reaction of 4-(hydroxymethyl)furan-2(5H)-one (4HM2F) with 21 carboxylic acids using polystyrene-carbodiimide (PS-carbodiimide) yielded an ester library. Four of the esters, (5-oxo-2,5-dihydrofuran-3-yl) methyl acetate (IS-1), (5-oxo-2,5-dihydrofuran-3-yl)methyl butyrate (IS-2), (5-oxo-2,5-dihydrofuran-3-yl)methyl 2-methylpropanoate (IS-3), and (5-oxo-2,5-dihydrofuran-3-yl)-methyl chloroacetate (IS-4), were tested as internal standards for the quantification of patulin in apple juice by gas chromatography-mass spectrometry in the selected ion monitoring mode (GC-MS-SIM). The developed method combines an AOAC official extractive step and a GC-MS-SIM analysis. Using a chromatographic column containing trifluoropropylmethylpolysiloxane as the stationary phase and IS-1 as the internal standard, it was possible to perform an accurate and precise quantification of underivatizated patulin in apple juice at concentrations down to 6 mug/L. A detection limit of 1 mug/L was established.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1883O – PubChem

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We outline a conceptual blueprint that provides direct and atom economical access to a wide range of complex polyheterocycles. Our method capitalizes on the ambiphilic reactivity of rhodacyclopentanones that arise upon exposure of cyclopropanes to Rh(I) catalysts and CO. Using this approach, a wide array of polycyclizations are achieved, including variants that involve powerful dearomatizations and medium ring formations.

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Benzofuran – Wikipedia,
Benzofuran | C8H2007O – PubChem

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The present invention provides 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts, and processes for preparing them, which have antagonism against excitatory amino acid receptors, in particular, an AMPA receptor. The 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts of the present invention are represented by formula (1) wherein Q, R, R 1and R 2are as described in the specification.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1702O – PubChem