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Editors: Karen Hindson, Haymo Ross; Deputy Editor: Natalia Ortúzar

Online ISSN: 2191-1363

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal

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March 05, 2014

Web of Knowledge Indexing

All articles in ChemistryOpen are now abstracted and indexed in Thomson-Reuters Web of Science. A first partial impact factor can be estimated from their data.

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    Room Temperature, Metal-Free Arylation of Aliphatic Alcohols

    Dr. Raju Ghosh, Erik Lindstedt, Dr. Nazli Jalalian and Prof. Berit Olofsson

    Article first published online: 11 APR 2014 | DOI: 10.1002/open.201402006

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    Easy, quick and green! Diaryliodonium salts are demonstrated as efficient arylating agents of aliphatic alcohols under mild and metal-free conditions. The reaction proceeds at room temperature within 90 min to give alkyl aryl ethers in good to excellent yields.

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    Building Blocks for the Construction of Bioorthogonally Reactive Peptides via Solid-Phase Peptide Synthesis

    Dr. Brian M. Zeglis, Fabien Emmetiere, Dr. Nagavarakishore Pillarsetty, Prof. Ralph Weissleder, Prof. Jason S. Lewis and Prof. Thomas Reiner

    Article first published online: 6 APR 2014 | DOI: 10.1002/open.201402000

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    The earlier, the better! We report a novel synthesis of tetrazine-functionalized artificial amino acids, the creation of a model tetrazine-containing pentapeptide using solid-phase peptide synthesis, and the facile and rapid bioorthogonal radiolabeling of this peptide using a 89Zr-desferrioxamine-labeled trans-cyclooctene.

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    Conformational Dynamics of DNA G-Quadruplex in Solution Studied by Kinetic Capillary Electrophoresis Coupled On-line with Mass Spectrometry

    Gleb G. Mironov, Dr. Victor Okhonin, Dr. Nasrin Khan, Dr. Christopher M. Clouthier and Prof. Dr. Maxim V. Berezovski

    Article first published online: 2 APR 2014 | DOI: 10.1002/open.201400002

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    Combining forces! Kinetic capillary electrophoresis is coupled on-line with mass spectrometry (KCE-MS) to study conformational dynamics of DNA G-quadruplexes in solution. Peak’s shift and its widening in KCE help measure rate and equilibrium constants; and ion mobility spectrometry (IMS) provides relative sizes, absolute molecular masses and stoichiometry.

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    N-Aryl Isoleucine Derivatives as Angiotensin II AT2 Receptor Ligands

    Dr. Malte Behrends, Dr. Charlotta Wallinder, Dr. Anna Wieckowska, Dr. Marie-Odile Guimond, Prof. Anders Hallberg, Prof. Nicole Gallo-Payet and Prof. Mats Larhed

    Article first published online: 13 MAR 2014 | DOI: 10.1002/open.201300040

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    Human not pig receptors! A series of benzamide substituted N-aryl isoleucine derivatives targeting the human AT2R have been synthesized. In this series, ligands with Ki values down to the single digit micromolar range have been identified. The presented data emphasize the importance of using human receptors in drug discovery programs.

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    Diastereoselective Additive Trifluoromethylation/Halogenation of Isoxazole Triflones: Synthesis of All-Carbon-Functionalized Trifluoromethyl Isoxazoline Triflones (pages 14–18)

    Dr. Hiroyuki Kawai, Yutaka Sugita, Etsuko Tokunaga, Hiroyasu Sato, Dr. Motoo Shiro and Prof. Dr. Norio Shibata

    Article first published online: 13 FEB 2014 | DOI: 10.1002/open.201300044

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    The SO2CF3 group acts three! Highly functionalized 5-trifluoromethyl-2-isoxazoline derivatives featuring a triflyl (SO2CF3) group at the 4-position were successfully synthesized via diastereoselective trifluoromethylation and halogenation of isoxazole triflones using the Ruppert–Prakash reagent. The triflyl group activates isoxazoles and the 4-position of CF3 adducts, and has a potential biological function.