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- 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.
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- You have full text access to this OnlineOpen articleUnderstanding E2 versus SN2 Competition under Acidic and Basic Conditions (pages 29–36)
Lando P. Wolters, Prof. Dr. Yi Ren and Prof. Dr. F. Matthias Bickelhaupt
Article first published online: 29 JAN 2014 | DOI: 10.1002/open.201300043
Titrating the LUMO: The character of the LUMO of a substrate CH3CH2−LG (LG=leaving group) is found to be pH dependent: whereas it is Cβ−H bonding under acidic conditions, it is Cβ−H antibonding under basic conditions. This is an important factor behind the corresponding shift in reactivity towards an electron-donating agent Nu from substitution to elimination.
- You have full text access to this OnlineOpen articleOne-Pot Synthesis and Applications of N-Heteroaryl Iodonium Salts (pages 19–22)
Dr. Marcin Bielawski, Joel Malmgren, Dr. Leticia M. Pardo, Ylva Wikmark and Prof. Berit Olofsson
Article first published online: 23 JAN 2014 | DOI: 10.1002/open.201300042
N-Heteroarylation: An efficient one-pot synthesis of N-heteroaryl iodonium triflates from the corresponding N-heteroaryl iodide has been developed. The reactivity and chemoselectivity of these iodonium salts were demonstrated by selectively introducing a pyridyl moiety onto both oxygen and carbon nucleophiles in good yields.