Naoko Ichiishi

Nature Chemistry. doi:10.1038/nchem.2672

Authors: Hongyin Gao, Zhe Zhou, Doo-Hyun Kwon, James Coombs, Steven Jones, Nicole Erin Behnke, Daniel H. Ess & László Kürti

The direct transfer of primary amino and hydroxyl groups to arylmetals in a scalable and environmentally friendly fashion remains a formidable synthetic challenge. Here, it is demonstrated that bench-stable N–H and N–alkyl oxaziridines can be used as efficient multifunctional reagents, without deprotonation, for the direct primary amination and hydroxylation of (hetero)arylmetals.

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Immunotherapy drugs have been hailed as a breakthrough in cancer treatment, but doctors are finding that what makes them effective is also what poses serious risks.

With climate policies in the crosshairs, companies pin hopes on job creation efforts

Nature Chemistry. doi:10.1038/nchem.2631

Authors: Juntao Ye, Zhihao Shi, Theresa Sperger, Yoshifumi Yasukawa, Cian Kingston, Franziska Schoenebeck & Mark Lautens

Existing methods for C–H activation depend on preinstalled directing groups, the removal of which poses a practical limitation on the use of these reactions in synthesis. Now, a remote-selective C−H alkylation reaction of arenes using an in situ generated spiropalladacycle has been shown to furnish benzofurans and indoles without the need for a directing group.

共和党のトランプ氏が勝利したアメリカ大統領選挙は、まだ開票作業が続いていますが、勝敗を決める選挙人の数で、トランプ氏が過半数を獲得した一方、全体の得票数は、これまでのところ民主党のクリントン氏が上回っていて、選挙人と得票の数が逆転する事態となっています。

Nature Chemistry. doi:10.1038/nchem.2585

Authors: Gang He, Gang Lu, Zhengwei Guo, Peng Liu & Gong Chen

Hampered by a lack of practical syntheses, benzazetidines are one of the few rarely explored compounds in N-heterocyclic chemical space. An efficient synthesis of various benzazetidines by Pd-catalysed intramolecular C−H amination of N-benzyl picolinamides is now reported. Reagent-controlled reductive elimination of a Pd intermediate is a key aspect of this particular method.

Nature Chemistry. doi:10.1038/nchem.2587

Authors: Eric C. Hansen, Dylan J. Pedro, Alexander C. Wotal, Nicholas J. Gower, Jade D. Nelson, Stephane Caron & Daniel J. Weix

Pharmaceutical compound libraries are an essential part of drug discovery and the screening of libraries for new drug leads is routine. It has now been shown that these heterocycle-rich, diverse libraries can also be used for ligand discovery. The discovery and application of several new ligands to nickel-catalysed cross-electrophile coupling is demonstrated.

Hundreds of photographers have gathered in Rio to follow the action in the Olympic arenas, swimming pools, racetracks, and more. Over the two weeks of the games, I’ll be featuring some amazing images from recent Olympic events. Today’s entry encompasses rowing, marathon swimming, sailing, weightlifting, steeple-chase, tennis, synchronized swimming, handball, wrestling, a marriage proposal, and much more.

Nature Chemistry. doi:10.1038/nchem.2571

Authors: Jorge A. Gonzalez, O. Maduka Ogba, Gregory F. Morehouse, Nicholas Rosson, Kendall N. Houk, Andrew G. Leach, Paul H.-Y. Cheong, Martin D. Burke & Guy C. Lloyd-Jones

The staged hydrolysis of N-methylimidodiacetic (MIDA) boronates is a prerequisite for their application in small-molecule constructions. Mechanistic studies now show that two distinct hydrolysis mechanisms operate in parallel, the partitioning — which is dependent on the pH, water activity and homogeneity of the medium — can be readily quantified by 18O incorporation.

Nature Chemistry. doi:10.1038/nchem.2554

Authors: Shigeki Kiyonaka, Ryou Kubota, Yukiko Michibata, Masayoshi Sakakura, Hideo Takahashi, Tomohiro Numata, Ryuji Inoue, Michisuke Yuzaki & Itaru Hamachi

The controlled activation of proteins inside living cells is an important goal in protein design research. Now, a strategy for allosteric activation using coordination chemistry has been demonstrated for two different kinds of neurotransmitter receptors, an ion-channel and a G-protein coupled glutamate receptor.

The chemical industry is dependent on the olefin/paraffin separation, which is mainly accomplished by using energy-intensive processes. We report the use of reticular chemistry for the fabrication of a chemically stable fluorinated metal-organic framework (MOF) material (NbOFFIVE-1-Ni, also referred to as KAUST-7). The bridging of Ni(II)-pyrazine square-grid layers with (NbOF5)2– pillars afforded the construction of a three-dimensional MOF, enclosing a periodic array of fluoride anions in contracted square-shaped channels. The judiciously selected bulkier (NbOF5)2– caused the looked-for hindrance of the previously free-rotating pyrazine moieties, delimiting the pore system and dictating the pore aperture size and its maximum opening. The restricted MOF window resulted in the selective molecular exclusion of propane from propylene at atmospheric pressure, as evidenced through multiple cyclic mixed-gas adsorption and calorimetric studies. Authors: A. Cadiau, K. Adil, P. M. Bhatt, Y. Belmabkhout, M. Eddaoudi

Cancer compounds from chemist Matthew Shair’s lab bring in $20 million

Thea Ekins-Coward lost an arm, local media report

Supported indium oxide catalyst could boost lab-scale process to an industrial level

Nature Chemistry. doi:10.1038/nchem.2439

Authors: Claudio Battilocchio, Florian Feist, Andreas Hafner, Meike Simon, Duc N. Tran, Daniel M. Allwood, David C. Blakemore & Steven V. Ley

The ability to form multiple carbon–carbon bonds in a controlled sequence represents an important goal in modern chemical synthesis. Here, the in situ preparation of reactive allylic and benzylic boronic acids, obtained by reacting flow-generated diazo compounds with boronic acids, and their application in controlled iterative C–C bond forming reactions is described.

Despite a well-developed and growing body of work in copper catalysis, the potential of copper to serve as a photocatalyst remains underexplored. Here we describe a photoinduced copper-catalyzed method for coupling readily available racemic tertiary alkyl chloride electrophiles with amines to generate fully substituted stereocenters with high enantioselectivity. The reaction proceeds at –40°C under excitation by a blue light-emitting diode and benefits from the use of a single, Earth-abundant transition metal acting as both the photocatalyst and the source of asymmetric induction. An enantioconvergent mechanism transforms the racemic starting material into a single product enantiomer. Authors: Quirin M. Kainz, Carson D. Matier, Agnieszka Bartoszewicz, Susan L. Zultanski, Jonas C. Peters, Gregory C. Fu

Author: Jake Yeston

In recent decades, transition-metal catalysis has become an indispensable tool in organic synthesis. Nevertheless, there remains a need for practical, safe, and efficient protocols for some transformations. A challenging example is nickelcatalyzed hydrocyanation (1), in which nonactivated olefins (alkenes) are converted to branched or linear nitriles through addition of hydrogen cyanide (HCN) (see the figure, panel A). This transformation is used industrially on a very large scale to produce adiponitrile, a key intermediate for Nylon-66 (see the figure, panel B). However, it is rarely used in laboratory or fine chemical syntheses because of safety concerns regarding HCN, an extremely toxic, volatile, and flammable agent. On page 832 of this issue, Fang et al. (2) report a method that avoids the use of HCN in the conversion of alkenes to nitriles and vice versa. Author: Hans-Günther Schmalz

Environment: Many industrial facilities report they are unaware of greener chemicals or alternative technology

Renewable Chemistry: Low-cost method for making key monomer enables a sugar-derived plastic for bottles

Collaboration: AstraZeneca, GSK, J&J combine with three universities to accelerate development of novel medicines