1450-90-4Relevant academic research and scientific papers
BF3·SMe2 for Thiomethylation, Nitro Reduction and Tandem Reduction/SMe Insertion of Nitrogen Heterocycles
S?derstr?m, Marcus,Zamaratski, Edouard,Odell, Luke R.
, p. 5402 - 5408 (2019/06/27)
Herein, a general, solvent-free and straightforward thiomethylation of electron deficient heterocycles using BF3·SMe2 as a dual thiomethyl source and Lewis acidic activator is presented. A range of heterocycles including pyrimidine, pyrazine, pyridazine, thiazole and purine derivatives were successfully substituted using this method. An unexpected reductive property of BF3·SMe2 towards nitropyridines was also discovered including an intriguing tandem reduction/SMe insertion process in certain substrates. Notable features of the present work include its convenience and use of a non-malodorous reagent while the discovery of novel chemical transformations using BF3·SMe2 provides fundamental new insights into the reactivity of this commonly employed reagent.
Palladium-Catalyzed Thiomethylation via a Three-Component Cross-Coupling Strategy
Wang, Ming,Qiao, Zongjun,Zhao, Jiaoyan,Jiang, Xuefeng
supporting information, p. 6193 - 6197 (2018/09/25)
In this report, the combination of masked inorganic sulfur and dimethyl carbonate was designed to achieve thiomethylated cross coupling of aryl chlorides. Remarkably, this powerful strategy realized thiomethylation of nucleosides bearing unprotected ribose, chloride-containing pharmaceuticals with late-stage coupling, and herbicides possessing multiple heteroatoms and steric hindrance. Moreover, this protocol is practically amenable to multigram-scale synthesis with a lower catalysis loading and a higher yield.
Methyl aryl thioether compound, and synthetic method and applications thereof
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Paragraph 0131; 0132; 0133, (2017/07/21)
The invention discloses a methyl aryl thioether compound represented by formula 2, and a synthetic method and applications thereof. According to the synthetic method, in a reaction solvent, an aryl halide or an aromatic halide, dimethyl carbonate, and potassium thioacetate are taken as reaction raw materials, reaction is carried out in the presence of metal palladium catalyst under the action of a ligand and an alkali so as to obtain the methyl aryl thioether compound. The reaction conditions of the synthetic method are mild; the raw materials are cheap and easily available; reaction operation is simple; yield is relatively high. The methyl aryl thioether compound can be used for providing skeleton structures for the synthesis of a plurality of natural products and medicines, and can be widely applied in industrialized large-scale production.
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page/Page column 26-27, (2011/09/14)
The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R2, R3, R4 and R5 are defined in the summary of the invention), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
[4,5']BIPYRIMIDINYL-6,4'-DIAMINE DERIVATIVES AS PROTEIN KINASE INHBITORS
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Page/Page column 23, 30, 31, 60-61, (2008/06/13)
The invention provides a novel class of compounds of the Formula (I): in which the symbols have the meanings given in the description and claims, to pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prev
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page/Page column 69, (2008/06/13)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page/Page column 36, (2008/06/13)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di
N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists.
Porter, John R,Archibald, Sarah C,Brown, Julien A,Childs, Kirstie,Critchley, David,Head, John C,Hutchinson, Brian,Parton, Ted A H,Robinson, Martyn K,Shock, Anthony,Warrellow, Graham J,Zomaya, Alex
, p. 1595 - 1598 (2007/10/03)
The SAR studies to optimise both potency and rate of clearance in the rat for a series of pyrimidine and pyridine based VLA-4 antagonists are described.
