38383-50-5Relevant academic research and scientific papers
Nickel-Catalyzed Reductive Cross-Coupling of Aryl Bromides with Vinyl Acetate in Dimethyl Isosorbide as a Sustainable Solvent
Su, Mincong,Huang, Xia,Lei, Chuanhu,Jin, Jian
supporting information, p. 354 - 358 (2022/01/15)
A nickel-catalyzed reductive cross-coupling has been achieved using (hetero)aryl bromides and vinyl acetate as the coupling partners. This mild, applicable method provides a reliable access to a variety of vinyl arenes, heteroarenes, and benzoheterocycles, which should expand the chemical space of precursors to fine chemicals and polymers. Importantly, a sustainable solvent, dimethyl isosorbide, is used, making this protocol more attractive from the point of view of green chemistry.
Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology
Heinrich, Timo,Sala-Hojman, Ada,Ferretti, Roberta,Petersson, Carl,Minguzzi, Stefano,Gondela, Andrzej,Ramaswamy, Shivapriya,Bartosik, Anna,Czauderna, Frank,Crowley, Lindsey,Wahra, Pamela,Schilke, Heike,B?pple, Pia,Dudek, ?ukasz,Le?, Marcin,Niedziejko, Paulina,Olech, Kamila,Pawlik, Henryk,W?oszczak, ?ukasz,Zuchowicz, Karol,Suarez Alvarez, Jose Ramon,Martyka, Justyna,Sitek, Ewa,Mikulski, Maciej,Szcz??niak, Joanna,J?ckel, Sven,Krier, Mireille,Król, Marcin,Wegener, Ansgar,Ga??zowski, Micha?,Nowak, Mateusz,Becker, Frank,Herhaus, Christian
, p. 11904 - 11933 (2021/09/02)
Due to increased lactate production during glucose metabolism, tumor cells heavily rely on efficient lactate transport to avoid intracellular lactate accumulation and acidification. Monocarboxylate transporter 4 (MCT4/SLC16A3) is a lactate transporter that plays a central role in tumor pH modulation. The discovery and optimization of a novel class of MCT4 inhibitors (hit 9a), identified by a cellular screening in MDA-MB-231, is described. Direct target interaction of the optimized compound 18n with the cytosolic domain of MCT4 was shown after solubilization of the GFP-tagged transporter by fluorescence cross-correlation spectroscopy and microscopic studies. In vitro treatment with 18n resulted in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. Moreover, pharmacokinetic properties of 18n allowed assessment of lactate modulation and antitumor activity in a mouse tumor model. Thus, 18n represents a valuable tool for investigating selective MCT4 inhibition and its effect on tumor biology.
Olefin Hydroarylation Catalyzed by a Single-Component Cobalt(-I) Complex
Suslick, Benjamin A.,Tilley, T. Don
supporting information, p. 1495 - 1499 (2021/03/03)
A single-component Co(-I) catalyst, [(PPh3)3Co(N2)]Li(THF)3, has been developed for olefin hydroarylations with (N-aryl)aryl imine substrates. More than 40 examples were examined under mild reaction conditions to afford the desired alkyl-arene product in good to excellent yields. Catalysis occurs in a regioselective manner to afford exclusively branched products with styrene-derived substrates or linear products for aliphatic olefins. Electron-withdrawing functional groups (e.g., -F, -CF3, and -CO2Me) were tolerated under the reaction conditions.
Olefination via Cu-Mediated Dehydroacylation of Unstrained Ketones
Dong, Guangbin,Xu, Yan,Zhou, Xukai
, p. 20042 - 20048 (2021/12/03)
The dehydroacylation of ketones to olefins is realized under mild conditions, which exhibits a unique reaction pathway involving aromatization-driven C-C cleavage to remove the acyl moiety, followed by Cu-mediated oxidative elimination to form an alkene between the α and β carbons. The newly adopted N′-methylpicolinohydrazonamide (MPHA) reagent is key to enable efficient cleavage of ketone C-C bonds at room temperature. Diverse alkyl- and aryl-substituted olefins, dienes, and special alkenes are generated with broad functional group tolerance. Strategic applications of this method are also demonstrated.
Nickel-Catalyzed Ligand-Free Hiyama Coupling of Aryl Bromides and Vinyltrimethoxysilane
Wei, Shichao,Mao, Yongjun,Shi, Shi-Liang
supporting information, p. 1670 - 1674 (2021/02/26)
We herein disclose the first Ni-catalyzed Hiyama coupling of aryl halides with vinylsilanes. This protocol uses cheap, nontoxic, and stable vinyltrimethoxysilane as the vinyl donor, proceeds under mild and ligand-free conditions, furnishing a diverse variety of styrene derivatives in high yields with excellent functional group compatibility.
COMPOUNDS FOR MODULATING DDAH AND ADMA LEVELS, AS WELL AS METHODS OF USING THEREOF TO TREAT DISEASE
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Page/Page column 110; 111; 112; 113; 115; 116, (2019/11/19)
Disclosed are compounds that can modulate DDAH and the amount of asymmetric dimethylarginine (ADMA) in a subject. Also provided are pharmaceutical compositions comprising these compounds, as well as methods of using these compositions to treat and/or prevent diseases associated with elevated or low levels of DDAH and ADMA.
PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST
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Paragraph 0099, (2017/07/29)
The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.
Selective electrocarboxylation of bromostyrene at silver cathode in DMF
Wang, Hui-Mei,Sui, Guo-Jiao,Wu, Di,Feng, Qiu,Wang, Huan,Lu, Jia-Xing
, p. 968 - 972 (2016/02/03)
The electroreduction behavior of bromostyrenes 1 in DMF has been detected by cyclic voltammetry (CV) on GC and Ag electrodes. Under the atmospheric pressure of CO2, selective electrocarboxylation of 1 was carried out in an undivided cell at Ag
Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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Page/Page column 46; 47, (2017/07/31)
The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)
Arylation of perfluoroalkyl vinyl sulfoxides via the Heck reaction
Sokolenko, Liubov V.,Yagupolskii, Yurii L.,Vlasenko, Yurii G.,Babichenko, Liudmila N.,Lipetskij, Volodimir O.,Anselmi, Elsa,Magnier, Emmanuel
supporting information, p. 1259 - 1262 (2015/03/04)
Heck reactions of perfluoroalkyl vinyl sulfoxides with aryl iodides are studied and palladium(II) acetate is shown to be the most convenient catalyst for this process. New E-1-aryl-2-perfluoroalkylsulfinylethylenes are synthesized. In all cases, by-products without a perfluoroalkylsulfinyl group are formed.
