76509-17-6Relevant academic research and scientific papers
Regioselective Single Electron Transfer Photocatalytic Synthesis of 2-Cyano-3-Ethylidenepiperidines. New Route to the Total Synthesis of (+/-) cis-Eburnamonine
Goes, Alexandre Da Silva,Ferroud, Clotilde,Santamaria, Jean
, p. 2235 - 2238 (1995)
A new synthesis of (+/-) cis-eburnamonine is described through a tetracyclic intermediate 3 obtained from 2-cyano-3-ethylidenepiperidines generated in situ by a regioselective single electron transfer (SET) photocatalysis.
Hydroarylation of Arenes via Reductive Radical-Polar Crossover
Flynn, Autumn R.,Mcdaniel, Kelly A.,Hughes, Meredith E.,Vogt, David B.,Jui, Nathan T.
supporting information, p. 9163 - 9168 (2020/07/10)
A photocatalytic system for the dearomative hydroarylation of benzene derivatives has been developed. Using a combination of an organic photoredox catalyst and an amine reductant, this process operates through a reductive radical-polar crossover mechanism where aryl halide reduction triggers a regioselective radical cyclization event, followed by anion formation and quenching to produce a range of complex spirocyclic cyclohexadienes. This light-driven protocol functions at room temperature in a green solvent system (aq. MeCN) without the need for precious metal-based catalysts or reagents or the generation of stoichiometric metal byproducts.
Novel protein kinase inhibitors related to tau pathology modulate tau protein-self interaction using a luciferase complementation assay
Holzer, Max,Schade, Nico,Opitz, Ansgar,Hilbrich, Isabel,Stieler, Jens,Vogel, Tim,Neukel, Valentina,Oberstadt, Moritz,Totzke, Frank,Schchtele, Christoph,Sippl, Wolfgang,Hilgeroth, Andreas
, (2018/09/26)
The current number of drugs available for the treatment of Alzheimer's disease (AD) is strongly limited and their benefit for therapy is given only in the early state of the disease. An effective therapy should affect those processes which mainly contribu
Ruthenium-Catalyzed Regioselective 1,4-Hydroboration of Pyridines
Kaithal, Akash,Chatterjee, Basujit,Gunanathan, Chidambaram
supporting information, p. 3402 - 3405 (2016/07/26)
Simple ruthenium precursor [Ru(p-cymene)Cl2]2 1 catalyzed regioselective 1,4-dearomatization of pyridine derivatives using pinacolborane is reported. Two catalytic intermediates, [Ru(p-cymene)Cl2Py] 2 and [Ru(p-cymene)Cls
First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators
Krug, Martin,Voigt, Burkhardt,Baumert, Christiane,Lüpken, Ralf,Molnár, Joséf,Hilgeroth, Andreas
experimental part, p. 2683 - 2688 (2010/07/09)
A series of 3-benzyloxy-1-aza-9-oxafluorenes has been synthesized and biologically evaluated as novel MDR modulators. The concentration dependent inhibition of the efflux pump ABCB1 (P-glycoprotein) has been characterized and is discussed in relation to calculated lipophilicity data. Instead of the molecular lipophilicity the exact positioning of functional groups was found decisive for the biological activities.
A simple Cu-catalyzed coupling approach to substituted 3-pyridinol and 5-pyrimidinol antioxidants
Nara, Susheel J.,Jha, Mukund,Brinkhorst, Johan,Zemanek, Tony J.,Pratt, Derek A.
experimental part, p. 9326 - 9333 (2009/04/06)
(Chemical Equation Presented) A convenient approach to 3-pyridinols and 5-pyrimidinols via a two-step Cu-catalyzed benzyloxylation/catalytic hydrogenation sequence is presented. The corresponding 3-pyridinamines and 5-pyrimidinamines can be prepared in an analogous sequence utilizing benzylamine in lieu of benzyl alcohol. The radical-scavenging ability of these derivatives are preliminarily explored and reveal that the increased acidities of the pyridinols and pyrimidinols render them susceptible to more significant kinetic solvent effects when compared to phenols.
HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES
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Page/Page column 68, (2008/06/13)
The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
BICYCLIC COMPOUNDS
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Page/Page column 47-48, (2010/02/14)
The present invention is to provide a bicyclic compound represented by the following formula: wherein Ring Q is pyridine or pyrimidine; Ring A is benzene or a heterocyclic ring; G is Ring B optionally having a substituent(s) R3, or an amino optionally substituted by one or two selected from the group consisting of alkyl(s), aralkyl(s) and cycloalkyl(s); Ring B is benzene, a heterocyclic ring, a cycloalkane or a cycloalkene; R1 is a group selected from the following formulae: R2 and R3 may be the same or different from each other, and each is cyano, nitro, etc.; m is 0, 1 or 2; R4 is hydrogen, a halogen, etc.; and R5 and R6 may be the same or different from each other, and each is hydrogen, an optionally substituted alkyl, etc., or a pharmaceutically acceptable salt thereof, which is a large conductance calcium-activated K channel opener useful for treatment of pollakiuria, urinary incontinence, etc.
3-`(HETERO) ARYLMETHOXY ! PYRIDINES AND THEIR ANALOGUES AS P38 MAP KINASE INHIBITORS
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Page/Page column 63-64; 66, (2010/11/30)
Compounds of the formula (I), wherein: -X=Y- is selected from -CR2=CR3- and -CR2=N-; R1 is selected from H, halo, NRR', NHC(=O)R, NHC(=O)NRR', NH2SO2R, and C(=O)NRR'; R2 and R3 (where present) are independently selected from H, optionally substituted C1-7 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, halo, amino, amido, hydroxy, ether, thio, thioether, acylamido, ureido and sulfonamino; R4 is an optionally substituted C5-20 aryl or C5-20 heteroaryl group; and R5 is selected from R5’, halo, NHR5’, C(=O)NHR5’, OR5’, SR5’, NHC(=O)R5’, NHC(=O)NHR5’, NHS(=O)R5’, wherein R5’ is H or C1-3 alkyl (optionally substituted by halo, NH2, OH, SH) are disclosed for use in therapy and for treating diseases ameliorated by inhibiting p38 MAP kinase.
Synthesis of substituted pyridines by the reactions of halopyridines with sulfur, oxygen and carbon nucleophiles under focused microwave irradiation
Cherng, Yie-Jia
, p. 4931 - 4935 (2007/10/03)
The nucleophilic substitution reactions of halopyridines with sulfur, oxygen and carbon nucleophiles under microwave irradiation was complete within several minutes with yields up to 99%. The method using microwave irradiation is superior to those conducted under conventional heating processes.
