- Ureido-containing benzimidazole derivative as well as preparation method and application thereof
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The invention discloses a ureido-containing benzimidazole derivative, whose structural general formula is shown as a formula (I). The invention also discloses a preparation method of the compound and application of the compound in the preparation of medicines for resisting chronic kidney diseases. The derivative is an inhibitor of selective homologous domain interacting protein kinase-2 (HIPK2), can lower the protein level of the HIPK2 at the same time to play a dual role, has an inhibition effect on the HIPK2 kinase and protein level, a fibrosis signal molecule smad3 and an inflammation signal molecule I[kappa]B-alpha phosphorylation level, can adjust the fibrosis and inflammation processes at the same time, and has a good market application prospect as chronic kidney disease treatment medicines.
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- Transition-metal-free synthesis of benzimidazoles mediated by KOH/DMSO
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Benzimidazoles are prepared by intramolecular N-arylations of amidines mediated by potassium hydroxide in DMSO at 120 °C. In this manner, diversely substituted products have been obtained in moderate to very good yields.
- Baars, Hannah,Beyer, Astrid,Kohlhepp, Stefanie V.,Bolm, Carsten
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p. 536 - 539
(2014/04/03)
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- A REGIOSELECTIVE COPPER CATALYZED SYNTHESIS OF BENZIMIDAZOLES AND AZABENZIMIDAZOLES
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The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N/-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N/-substituted amides. The process is useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
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Page/Page column 34
(2009/03/07)
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- Copper-catalyzed synthesis of benzimidazoles via cascade reactions of o-haloacetanilide derivatives with amidine hydrochlorides
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(Chemical Equation Presented) We have developed an efficient method for the synthesis of benzimidazoles via cascade reactions of o-haloacetoanilide derivatives with amidine hydrochlorides. The protocol uses 10 mol % CuBr as the catalyst, CS2CO
- Yang, Daoshan,Fu, Hua,Hu, Liming,Jiang, Yuyang,Zhao, Yufen
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p. 7841 - 7844
(2008/12/22)
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- NITROGEN-CONTAINING HETEROCYCLE DERIVATIVE AND ORGANIC ELECTROLUMINESCENT ELEMENT USING THE SAME
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A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.
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Page/Page column 38
(2010/02/14)
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