- Synthesis of 2,5-dibromobenzaldehyde and its reaction with hexylmagnesium bromide
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2,5-Dibromobenzaldehyde (3) is synthesized by the oxidation of 2,5-dibromotoluene (1) via 2,5-dibromobenzylidene diacetate (2). Grignard reaction of hexylmagnesium bromide with 2 gives the normal addition product, 2,5-dibromo-α-hexylbenzyl alcohol (5) and
- Shimura,Kawai,Minegishi
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- Strategy for Overcoming Full Reversibility of Intermolecular Radical Addition to Aldehydes: Tandem C-H and C-O Bonds Cleaving Cyclization of (Phenoxymethyl)arenes with Carbonyls to Benzofurans
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An intermolecular addition of carbon radicals enabled by a cascade radical coupling strategy is developed. It includes an intermolecular alkyl radical addition to a carbonyl group followed by an intramolecular alkoxy radical addition to haloarenes and produces substituted benzofurans in high yields. The radical nature of this reaction is explored by radical trapping experiments and EPR analysis. The mechanism is investigated by KIE experiments and control experiments. This method could provide rapid and practical access to the key intermediate of TAM-16, a safe and potent antibacterial agent for treating tuberculosis, and, therefore, is of great importance for organic synthesis and the pharmaceutical industry.
- Zheng, Hong-Xing,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
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supporting information
p. 3310 - 3313
(2018/06/11)
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- ALDOSTERONE SYNTHASE INHIBITORS
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The present invention relates to compounds of the formulas (IA) and (IB) and pharmaceutically acceptable salts thereof, wherein A and R1 - R6, are as defined herein. The invention also relates to pharmaceutical compositions comprisin
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Page/Page column 61
(2016/06/28)
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- Synthesis of oligophenylenevinylene heptamers substituted with fullerene moieties
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Oligophenylenevinylene (OPV) derivatives substituted with one or two fullerene subunits have been prepared starting from a fullerene carboxylic acid derivative and OPV heptamers bearing one or two alcohol functions. The electrochemical properties of the resulting C60-OPV derivatives have been investigated by cyclic voltammetry. Whereas the fist reduction of both C60-OPV conjugates is centered on the C60 unit, the oxidation is centered on the OPV rod. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Gegout, Aline,Holler, Michel,Figueira-Duarte, Teresa M.,Nierengarten, Jean-Francois
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experimental part
p. 3627 - 3634
(2009/04/07)
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- Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity
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The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines, as well as by cellular stresses including chemotoxins, peroxides, and irradiation. They have been implicated in the pathology of a variety of different diseases with an inflammatory component including asthma, stroke, Alzheimer's disease, and type 2 diabetes mellitus. In this work, high-throughput screening identified a JNK inhibitor with an excellent kinase selectivity profile. Using X-ray crystallography and biochemical screening to guide our lead optimization, we prepared compounds with inhibitory potencies in the low-double-digit nanomolar range, activity in whole cells, and pharmacokinetics suitable for in vivo use. The new compounds were over 1000-fold selective for JNK-1 and -2 over other MAP kinases including ERK2, p38α, and p38δ and showed little inhibitory activity against a panel of 74 kinases.
- Szczepankiewicz, Bruce G.,Kosogof, Christi,Nelson, Lissa T. J.,Liu, Gang,Liu, Bo,Zhao, Hongyu,Serby, Michael D.,Xin, Zhili,Liu, Mei,Gum, Rebecca J.,Haasch, Deanna L.,Wang, Sanyi,Clampit, Jill E.,Johnson, Eric F.,Lubben, Thomas H.,Stashko, Michael A.,Olejniczak, Edward T.,Sun, Chaohong,Dorwin, Sarah A.,Haskins, Kristi,Abad-Zapatero, Cele,Fry, Elizabeth H.,Hutchins, Charles W.,Sham, Hing L.,Rondinone, Cristina M.,Trevillyan, James M.
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p. 3563 - 3580
(2007/10/03)
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