929074-45-3Relevant academic research and scientific papers
Annelated Pyridine Bases for the Selective Acylation of 1,2-Diols
Mayr, Stefanie,Zipse, Hendrik
supporting information, (2022/03/08)
A set of 24 annelated derivatives of 4-diaminopyridine (DMAP) has been synthesized and tested with respect to its catalytic potential in the regioselective acylation of 1,2-diol substrates. The Lewis basicities of the catalysts as quantified through quantum chemical calculations vary due to inductive substituent effects and intramolecular stacking interactions between side chain π-systems and the pyridinium core ring system. The primary over secondary hydroxyl group selectivities in catalytic acylations of 1,2-diol substrates depend on the size and the steric demand of the Lewis base and the anhydride reagent.
2,3-DISUBSTITUTED PYRIDO[3,4-B]PYRAZINE-CONTAINING COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0067-0069, (2022/01/06)
The present invention generally relates to 2,3-Disubstituted pyrido[3,4- b]pyrazine-containing compounds as a kinase inhibitor and methods of uses thereof. Pharmaceutical compositions and methods for treating those kinase related diseases are within the scope of this invention.
BIARYL DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 0313; 0314, (2018/08/07)
Provided is a compound showing excellent antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C=O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.
PHARMACEUTICALS COMPRISING BIARYL DERIVATIVES OR SALTS THEREOF
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Paragraph 0307; 0308; 0309, (2018/10/24)
PROBLEM TO BE SOLVED: To provide compounds with excellent antimycotic activity against Trichophyton. SOLUTION: The invention provides pharmaceuticals comprising biaryl derivatives represented by general formula (I) or salts thereof, where ring A is optionally substituted phenyl or the like; Q is CH2 or the like; X1, X2 and X3 are CR1 or the like; and Y is CH or N. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
Annelated pyridines as highly nucleophilic and Lewis basic catalysts for acylation reactions
Tandon, Raman,Unzner, Teresa,Nigst, Tobias A.,De Rycke, Nicolas,Mayer, Peter,Wendt, Bernd,David, Olivier R. P.,Zipse, Hendrik
supporting information, p. 6435 - 6442 (2013/07/05)
New heterocyclic derivatives of 9-azajulolidine have been synthesized and characterized with respect to their nucleophilicity and Lewis basicity. The Lewis basicity of these bases as quantified through their theoretically calculated methyl-cation affinities correlate well with the experimentally measured reaction rates for addition to benzhydryl cations. All newly synthesized pyridines show exceptional catalytic activities in benchmark acylation reactions, which correlate only poorly with Lewis basicity or nucleophilicity parameters. A combination of Lewis basicity with charge and geometric parameters in the framework of a three-component quantitative structure-activity relationship (QSAR) model is, however, highly predictive. Copyright
