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# Organic Chemistry # Synthesis of isoquinolines from benzimidates and alkynes via cobalt(III)-catalyzed C-H functionalization/cyclizationThe Journal of Organic Chemistry Publication Date (Web): June 30, 2017 DOI: 10.1021/acs.joc.7b01052 Shasha GONG, Wanlin Xi, Zhenhua DING, and Haiying Sun Abstract: C-H alkenylation/annulation of benzimidates with alkynes has been realized by Cp*Co(III) catalyst under air. A series substituted isoquinolines were obtained with moderate to good yields under mild reaction conditions. Link to CBG： http://www./news/art?id=4284 Link to the paper： http://pubs./doi/10.1021/acs.joc.7b01052 # Medicinal Chemistry # Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid TumorsJournal of Medicinal Chemistry Publication Date (Web): June 30, 2017 DOI: 10.1021/acs.jmedchem.7b00360 Ken A. Brameld, Timothy D Owens, Erik Verner, Eleni Venetsanakos, J. Michael Bradshaw, Vernon T Phan, Danny Tam, Kwan H. Leung, Jin Shu, Jacob LaStant, David G Loughhead, Dane E Karr, Mary E Gerritsen, David Michael Goldstein, and Jens Oliver Funk Abstract: Aberrant signaling of the FGF/FGFR pathway occurs frequently in cancers and is an oncogenic driver in many solid tumors. Clinical validation of FGFR as a therapeutic target has been demonstrated in bladder, liver, lung, breast, and gastric cancers. Our goal was to develop an irreversible covalent inhibitor of FGFR1-4 for use in oncology indications. An irreversible covalent binding mechanism imparts many desirable pharmacological benefits including high potency, selectivity, and prolonged target inhibition. Herein we report, the structure-based design, medicinal chemistry optimization and unique ADME assays of our irreversible covalent drug discovery program which culminated in the discovery of compound 34 (PRN1371), a highly selective and potent FGFR1-4 inhibitor. Link to CBG： http://www./news/art?id=4286 Link to the paper： http://pubs./doi/10.1021/acs.jmedchem.7b00360 # Catalysis # Ni3FeN Supported Fe3Pt Intermetallic Nanoalloy as a High Performance Bifunctional Catalyst for Metal-Air BatteryAngewandte Chemie International Edition Accepted manuscript online: 30 June 2017 DOI: 10.1002/anie.201705778 Zhiming Cui, Gengtao Fu, Yutao Li, John B. Goodenough Abstract: Electrocatalysts for both the oxygen reduction and evolution reactions (ORR and OER) are vital for the performances of rechargeable metal-air batteries. Herein, we report an advanced bifunctional oxygen electrocatalyst consisting of porous metallic Nickel-iron nitride (Ni3FeN) supporting ordered Fe3Pt intermetallic nanoalloy. In this hybrid catalyst, the bimetallic nitride Ni3FeN mainly contributes to the high activity for the OER while ordered Fe3Pt nanoalloy contributes to the excellent activity for the ORR. Robust Ni3FeN supported Fe3Pt catalysts show superior catalytic performance to the state of the art ORR catalyst (Pt/C) and OER catalyst (Ir/C). Fe3Pt/Ni3FeN bifunctional catalyst enables Zn-air batteries to achieve a long-term cycling performance of over 480 h at 10 mA cm−2 with high efficiency. The extraordinarily high performance of Fe3Pt/Ni3FeN bifunctional catalyst makes it a very promising air cathode in alkaline electrolyte. Link to CBG： http://www./news/art?id=4176 Link to the paper： http://onlinelibrary./doi/10.1002/anie.201705778/full 了解更多最全、最新论文快讯 登录CBG官网（www.） 下载ChemBeanGo APP CBG资讯 ∣知识就是力量 |
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