76240-19-2Relevant academic research and scientific papers
PHTHALAZINE DERIVATIVES, AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Paragraph 0278, (2018/11/21)
The present invention provides a compound of formula I, a cis-trans isomer, an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, or a pharmaceutical acceptable salt and ester thereof, a preparation method for preparing the same, a pharmaceutical composition comprising the same and a use of the compound as an α5-GABAA receptor regulator, wherein T, Z, A and Y are as defined in the description.
Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines
Moszczyński-P?tkowski, Rafa?,Majer, Jakub,Borkowska, Ma?gorzata,Bojarski, ?ukasz,Janowska, Sylwia,Mat?oka, Miko?aj,Stefaniak, Filip,Smuga, Damian,Bazyd?o, Katarzyna,Dubiel, Krzysztof,Wieczorek, Maciej
, p. 96 - 116 (2018/06/06)
New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.
Metal-free michael-addition-initiated three-component reaction for the regioselective synthesis of highly functionalized pyridines: Scope, mechanistic investigations and applications
Allais, Christophe,Lieby-Muller, Frederic,Rodriguez, Jean,Constantieux, Thierry
supporting information, p. 4131 - 4145 (2013/07/19)
A metal-free and completely regioselective three-component synthesis of highly functionalized pyridines from 1,3-dicarbonyl derivatives and Michael acceptors has been achieved. Activated Michael acceptors, that is, β,γ-unsaturated α-oxo carbonyl derivatives, were utilized, allowing substitution at the 4-position and remarkable functional diversity at the 2-position of the pyridine ring. The scope and limitations of this environmentally friendly domino reaction are disclosed, with full experimental data, and the results of mechanistic investigations are discussed. The three-component synthesis of polysubstituted pyridines starting from 1,3-dicarbonyl compounds, α,β-unsaturated carbonyl derivatives and ammonium acetate has been studied, including the scope and mechanism. This methodology is a rare example of a totally regioselective multicomponent access to highly substituted pyridines that complies with many of the stringent criteria of sustainable chemistry. Copyright
MONOBACTAMS
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Page/Page column 68, (2012/06/16)
The present invention is directed to a new class of monobactam derivatives and their use for treating bacterial infections.
PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR
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Page/Page column 52, (2009/10/30)
The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof
SYNTHESIS OF 2-ARYL PYRIMIDINE 4-CARBOXYLIC ACID AMIDES
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Page 27; 2, (2010/02/09)
Disclosed is a method for the preparation of 2-aryl pyrimidine 4 carboxylic acid amides by reacting an aryl carboxamidine with a 4 substituted 2-oxo-3-butenyl amide. Also disclosed is a method for the preparation of 2-aryl pyrimidine 4 carboxylic acid ami
