95384-59-1Relevant academic research and scientific papers
Copper-catalyzed regioselective 2-amination of o-haloanilides with aqueous ammonia
Tang, Yan-Ling,Li, Mei-Ling,Gao, Jin-Chun,Sun, Yun,Qu, Lu,Huang, Feng,Mao, Ze-Wei
supporting information, (2021/04/02)
An efficient Cu(II)-vasicine catalytic system has been developed for intramolecular C[sbnd]N bond formation. In this way, regioselective 2-amination of o-haloanilides with aqueous ammonia in EtOH has been achieved. This strategy provides several advantages, such as good regioselectivity, high yields and functional group tolerance.
Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators
Charton, Julie,Girault-Mizzi, Sophie,Debreu-Fontaine, Marie-Ange,Foufelle, Fabienne,Hainault, Isabelle,Bizot-Espiard, Jean-Guy,Caignard, Daniel-Henri,Sergheraert, Christian
, p. 4490 - 4518 (2007/10/03)
Design, synthesis and structure-activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. AMPK is the central component of a protein kinase cascade that plays a key role in the regulation of energy balance. Once activated, AMPK initiates a series of responses that are aimed at restoring the energy balance of the cell and recent studies have indicated that AMPK plays an important role in regulation of the whole-body energy metabolism. The following study based on the lead compound S27847 involved modification of three regions of this compound. Preliminary structure-activity relationships are being described.
Conversion of sterically hindered diacylated 1,2-phenylenediamines into 2-substituted benzimidazoles
Charton, Julie,Girault-Mizzi, Sophie,Sergheraert, Christian
, p. 492 - 497 (2007/10/03)
A series of bulky 2-substituted benzimidazoles was designed in order to find new leads for several biological targets. Formation by cyclodehydration from their monoacylated counterparts was shown to be strongly dependent upon the nature of the acyl group. In the case of a dicyclohexylmethyl group, cycllzation was only observed in a p-toluenesulfonic acid/toluene mixture from the symmetrical diacylated precursor. Analysis of the mechanism was begun starting from mixed diacylated derivatives.
Composition and method for dyeing dye-susceptible material
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Page/Page column 12, (2008/06/13)
Composition for colouring dye-susceptible material (preferably keratinous material), containing at least one pro-dye (especially a glutaramide) and at least one enzyme capable of reacting, cleaving, or modifying the enzymatically-labile functionality in the pro-dye to form a dye substance or a direct dye; as well as a 2-component-kit.
SOLID-PHASE REACTIONS OF AROMATIC AMINES WITH CARBOXYLIC ACIDS UNDER CONDITIONS OF SHEAR DEFORMATION AND HIGH PRESSURE
Leont'ev, A. I.,Zharov, A. A.,Chistotina, N. P.
, p. 1680 - 1684 (2007/10/02)
Solid mixtures of carboxylic acids and aromatic amines react under shear deformation at high pressure (to 8 GPa) for form amides, in the case of ortho-phenylenediamine-substituted benzimidazoles are formed.Under these conditions the conversion rates are hundreds of thousands of times higher than when the same processes are carried out in liquid phase.The cyclization reaction is accelerated to a lesser degree than the reaction of formation of the corresponding amide.The increase of the length of the carboxylic acid radical prevents the cyclization reaction. Keywords: shear deformation, high pressure, aromatic amines, carboxylic acids, amide, benzimidazole, amidization, cyclization.
