13 research outputs found

    Copper Catalyzed Cross-Coupling of Iodobenzoates with Bromozinc-difluorophosphonate

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    A copper-catalyzed cross-coupling of iodobenzoates with bromozinc-difluorophosphonate, generated from diethyl bromodifluoromethylphosphonate and zinc in dioxane, is reported. The notable features of this reaction are its high reaction efficiency, excellent functional group compatibility, and operational simplicity. This protocol provides a useful and facile access to aryldifluorophosphonates of interest in life science

    Access to Difluoromethylated Arenes by Pd-Catalyzed Reaction of Arylboronic Acids with Bromodifluoroacetate

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    An unprecedented example of Pd-catalyzed difluoromethylation of aryl boronic acids with bromodifluoroacetate is described. The reaction proceeds under mild reaction conditions with hydroquinone and Fe­(acac)<sub>3</sub> as additives. Preliminary mechanistic studies reveal that a difluorocarbene pathway is involved in the reaction, which is unusual compared to the most traditional approaches. This reaction has advantages of high efficiency and excellent functional group compatibility, even toward bromide and hydroxy group, thus providing a useful protocol for drug discovery and development

    Heteroaryldifluoromethylation of Organoborons Catalyzed by Palladium: Facile Access to Aryl(Heteroaryl)difluoromethanes

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    A first example of Pd-catalyzed heteroaryldifluoromethylation of organoborons with bromodifluoromethylated heteroarenes has been described. The use of phosphine ligand PAd<sub>2</sub>(<i>n</i>-Bu)·HI is critical for the reaction efficiency. With use of this ligand, a wide range of aryl­(heteroaryl)­difluoromethanes were obtained with high efficiency. The notable features of this reaction are its broad substrate scope and excellent functional group compatibility, thus providing a facile protocol for application in drug discovery and development

    Nickel-Catalyzed Reductive Cross-Coupling of (Hetero)Aryl Iodides with Fluorinated Secondary Alkyl Bromides

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    A mild and efficient nickel-catalyzed reductive cross-coupling between fluorinated secondary alkyl bromides and (hetero)­aryl iodides is described. The use of FeBr<sub>2</sub> as an additive successfully overcomes the hydrodebromination and β-fluorine elimination of fluorinated substrates and allows the efficient synthesis of a wide range of trifluoromethyl and difluoroalkyl containing aliphatic compounds with a fluoroalkyl substituted tertiary carbon center. The notable features of this protocol are the synthetic and operational simplicity without preparation of moisture sensitive organometallic reagents and excellent functional group compatibility, even toward active proton containing substrates

    Highly Selective <i>gem</i>-Difluoroallylation of Organoborons with Bromodifluoromethylated Alkenes Catalyzed by Palladium

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    A first example of Pd-catalyzed <i>gem</i>-difluoroallylation of organoborons using 3-bromo-3,3-difluoropropene (BDFP) in high efficiency with high α/γ-substitution regioselectivity has been developed. The reaction can also be extended to substituted BDFPs and has advantages of low catalyst loading (0.8 to 0.01 mol %), broad substrate scope, and excellent functional group compatibility, thus providing a facile route for practical application in drug discovery and development

    Pd-Catalyzed Dehydrogenative Cross-Coupling of Polyfluoroarenes with Heteroatom-Substituted Enones

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    The first example of intermolecular regioselective α-arylation of heteroatom-substituted enones with polyfluoroarenes via twofold C–H bond functionalization using a palladium catalyst is reported. This approach provides rapid access to a wide range of α-fluoroarylated enones of interest in life science

    Pd-Catalyzed Dehydrogenative Cross-Coupling of Polyfluoroarenes with Heteroatom-Substituted Enones

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    The first example of intermolecular regioselective α-arylation of heteroatom-substituted enones with polyfluoroarenes via twofold C–H bond functionalization using a palladium catalyst is reported. This approach provides rapid access to a wide range of α-fluoroarylated enones of interest in life science

    Segregation analysis of EC in an extended pedigree of Taihang.

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    <p>-: Parameter at this value is not estimated.</p><p>a: See <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0009668#s2" target="_blank">Materials and Methods</a> for definitions of the parameters.</p><p>b: Parameter estimate went to bound.</p

    Segregation analysis of oesophageal cancer in two large pedigrees of Chaoshan.

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    <p>-: Parameter at this value is not estimated.</p><p>a: See <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0009668#s2" target="_blank">Materials and Methods</a> for definitions of the parameters.</p><p>b: Parameter estimate went to bound.</p
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