131747-60-9Relevant articles and documents
Oxidation of methyl heteroaryls with molecular oxygen: A facile synthesis of 2-[N-(tert-butoxycarbonyl)amino]-4-pyridinecarbaldehyde
Berlin, Michael,Aslanian, Robert,Ruiz, Manuel De Lera,McCormick, Kevin D.
, p. 2529 - 2533 (2007)
Oxidation of nitrogen-based methyl heteroaryls with molecular oxygen resulted in the formation of the corresponding benzyl alcohols. While experimentally easy and amenable to large-scale preparations, this approach has limitations with respect to the particular nature of heterocyclic substrates. Using this methodology, the title compound, 2-[N-(tert-butoxycarbonyl)amino]-4- pyridinecarbaldehyde, considered to be a versatile pharmaceutical intermediate, was prepared on a multigram scale. Georg Thieme Verlag Stuttgart.
Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: New multimodal fluorinated and iodinated radiotracers
Maisonial, Aurélie,Kuhnast, Bertrand,Papon, Janine,Boisgard, Rapha?l,Bayle, Martine,Vidal, Aurélien,Auzeloux, Philippe,Rbah, Latifa,Bonnet-Duquennoy, Mathilde,Miot-Noirault, Elisabeth,Galmier, Marie-Josèphe,Borel, Michèle,Askienazy, Serge,Dollé, Frédéric,Tavitian, Bertrand,Madelmont, Jean-Claude,Moins, Nicole,Chezal, Jean-Michel
experimental part, p. 2745 - 2766 (2011/06/24)
This study reports a series of 14 new iodinated and fluorinated compounds offering both early imaging (123I, 124I, 18F) and systemic treatment (131I) of melanoma potentialities. The biodistribution of each 125I-labeled tracer was evaluated in a model of melanoma B16F0-bearing mice, using in vivo serial γ scintigraphic imaging. Among this series, [125I]56 emerged as the most promising compound in terms of specific tumoral uptake and in vivo kinetic profile. To validate our multimodality concept, the radiosynthesis of [18F]56 was then optimized and this radiotracer has been successfully investigated for in vivo PET imaging of melanoma in B16F0- and B16F10-bearing mouse model. The therapeutic efficacy of [131I]56 was then evaluated in mice bearing subcutaneous B16F0 melanoma, and a significant slow down in tumoral growth was demonstrated. These data support further development of 56 for PET imaging (18F, 124I) and targeted radionuclide therapy ( 131I) of melanoma using a single chemical structure.
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Mitchell, Michael L.,Son, Jong Chan,Lee, Ill Young,Lee, Chong-Kyo,Kim, Hae Soo,Guo, Hongyan,Wang, Jianhong,Hayes, Jaclyn,Wang, Michael,Paul, Amber,Lansdon, Eric B.,Chen, James M.,Eisenberg, Gene,Geleziunas, Romas,Xu, Lianhong,Kim, Choung U.
scheme or table, p. 1585 - 1588 (2010/06/17)
A series of N1-heterocyclic pyrimidinediones were extensively evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Inhibitor 1 is active against NNRTI-resistant viruses including RT mutant K103N. The co-crystal structure of inhibit
Labelled analogues of halobenzamides as multimodal radiopharmaceuticals and their precursors
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Page/Page column 26, (2009/08/16)
The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen atom, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group
Novel HIV reverse transcriptase inhibitors
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Page/Page column 37-38, (2008/06/13)
The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
CYCLOALKANOPYRIDINE DERIVATIVE
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, (2010/11/24)
Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.
Substituted benzimidazoles
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, (2008/06/13)
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
Efficient pyridinylmethyl functionalization: Synthesis of 10,10-bis[(2-fluoro-4-pyridinyl)methyl]-9(10H)-anthracenone (DMP 543), an acetylcholine release enhancing agent
Pesti,Huhn,Yin,Xing,Fortunak,Earl
, p. 7718 - 7722 (2007/10/03)
2-Fluoro-4-methylpyridine (3) is efficiently functionalized by chlorination, hydrolysis and methane-sulfonylation into the novel alkylating agent 7. This mesylate is used for the bisalkylation of anthrone under carefully defined conditions to prepare the cognition enhancer drug candidate 1. This process proceeds in up to 37% overall yield and is adaptable for large scale synthesis.