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- You have full text access to this OnlineOpen articleRoom 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
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.
- You have full text access to this OnlineOpen articleBuilding 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
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.
- You have full text access to this OnlineOpen articleConformational 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
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.
- You have full text access to this OnlineOpen articleN-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
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.
- You have full text access to this OnlineOpen articleDiastereoselective 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
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.