29027-20-1Relevant articles and documents
Ligand Promoted meta-C-H Chlorination of Anilines and Phenols
Shi, Hang,Wang, Peng,Suzuki, Shin,Farmer, Marcus E.,Yu, Jin-Quan
, p. 14876 - 14879 (2016)
Pd-catalyzed meta-C-H chlorination of anilines and phenols is developed using norbornene as the mediator. Heterocycles, including indole, thiophene, and indazole, are tolerated. The identification of a new pyridone-based ligand is crucial for the success of this meta-C-H chlorination reaction. Subsequent diverse transformations of the chlorinated products demonstrate the versatility of meta-C-H chlorination.
Fe2O3/NGr@C- and Co-Co3O4/NGr@C-catalysed hydrogenation of nitroarenes under mild conditions
Formenti, Dario,Topf, Christoph,Junge, Kathrin,Ragaini, Fabio,Beller, Matthias
, p. 4473 - 4477 (2016/07/06)
An improved hydrogenation of nitroarenes using nano-structured iron- and cobalt-based catalysts is presented. Modifications of the heterogeneous catalysts by N-doped graphene-flakes are crucial for the success of selective reductions. The use of polar solvents and basic additives has a significant positive influence on the rate of reduction of nitroarenes. This allows performing non-noble metal-catalysed hydrogenations under very mild reaction conditions (e.g. 70 °C and 20 bar). On the basis of the obtained catalytic results a heterolytic mechanism for the hydrogenation process is postulated, too.
FACTOR IXA INHIBITORS
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Page/Page column 41, (2016/11/07)
The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, trans
IMPROVED MODULATORS OF HEC1 ACTIVITY AND METHODS THEREFOR
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Paragraph 00358, (2013/06/27)
Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases
Modulators Of HEC1 Activity And Methods Therefor
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Page/Page column 31-32, (2011/10/10)
Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.
NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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Page/Page column 137, (2008/12/07)
The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.
Process for preparing 3-chloro-5-nitrotoluene
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Page 2, (2008/06/13)
A preparation process of 3-chloro-5-nitrotoluene is provided in mild conditions. It is a process for preparing 3-chloro-5-nitrotoluene, which comprises reacting 2-methyl-4-nitroaniline with a chlorinating agent such as 5-butyl hypochlorite in a neutral co
Synthesis and structure - Activity relationships of chiral allosteric modifiers of hemoglobin
Grella,Danso-Danquah,Safo,Joshi,Kister,Marden,Hoffman,Abraham
, p. 4726 - 4737 (2007/10/03)
A series of allosteric effectors of hemoglobin, 2-(aryloxy)-2-alkanoic acids, was prepared to investigate the effect of the stereocenter on allosteric activity. The chiral analogues were based on the lead compound, RSR13 (3b), with different alkyl/alkanoic and cycloalkyl/cycloalkanoic groups positioned at the acidic chiral center. Of the 23 racemic molecules synthesized, 5 were selected for resolution based on structure - activity relationships. One chiral analogue, (-)-(1R,2R)-1-[4-[[(3,5-dimethylanilino)carbonyl]methyl]phenoxy]-2-methylcycl opentanecarboxylic acid (11), exhibited greater in vitro activity in hemoglobin solutions than its antipode, racemate, and RSR13. Compound (-)-(1R,2R)-11 was equipotent with RSR13 in whole blood, is a candidate for in vivo animal studies, and if efficacious and safe has a potential for use in humans. In general, it was found that chirality affects allosteric effector activity with measurable differences observed between enantiomers and the racemates.
Pyridazinedione compounds useful in treating neurological disorders
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, (2008/06/13)
The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
The Kinetics of the Reactions of Picryl Chloride with Some Substituted Anilines. Part 5.
Emokpae, Thomas A.,Eguavoen, Osa,Hirst, Jack
, p. 829 - 831 (2007/10/02)
Arrhenius parameters have been measured for the reactions of picryl chloride with the following substituted anilines in acetonitrile: 3-amino- and 3-methyl-aniline, 3-amino-5-nitroaniline, 3-fluoro-5-methylsulphonylaniline, 3-X-5-methylanilines (X=NO2, OMe, CH3, F, Cl, Br, or I) and 3,5-X2-anilines (X = F, Cl, Br, or I).A total of 33 3,5-disubstituted anilines have now been examined for the additivity of substituent effects on the free energy of activation, and it has been shown that with the exception of 3-amino-5-nitroaniline this hypothesis reproduces experimental rate constants within a factor of 2.A rationalization is proposed for the deviations that occur in some cases when more stringent criteria of additivity are used.