60418-33-9Relevant academic research and scientific papers
Applicability aspects of transition metal-catalyzed aromatic amination protocols in medicinal chemistry
Tasler, Stefan,Mies, Jan,Lang, Martin
, p. 2286 - 2300 (2008/09/19)
The application of palladium- and coppercatalyzed reactions for the aromatic amination of pharmacologically relevant scaffolds is investigated. The focus is set on the scope of several protocols for the introduction of amines of broad structural diversity, allowing for the synthesis of numerous derivatives of one biological hit structure for screening in biological assay systems. Thus, attaining optimized yields and TONs had not a major priority, most important were practical aspects, that is no further purification and drying of reagents and solvents had to be envisaged, ideally only a few transition metalbased protocols had to be applied for synthesizing structurally diverse compounds in sufficient amounts (several milligrams) for screening without any finetuning of conditions and catalytic systems.
Nitro-substituted phenyl-piperazine compounds, their preparation and use in medicaments
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Page/Page column 72, (2008/06/13)
The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitre-substituted ph
SUBSTITUTED PHENYL-PIPERAZINE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS
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Page/Page column 108, (2008/06/13)
The present invention relates to substituted phenyl-piperazine compounds of general formula (I), a process for their preparation, medicaments comprising said substituted phenyl-piperazine compounds as well as the use of said substituted phenyl-piperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
Competitive Cyclisations of Singlet and Triplet Nitrenes. Part 8. The 1-(2-Nitrenophenyl)pyrazoles and Related Systems
Lindley, John M.,McRobbie, Ian M.,Meth-Cohn, Otto,Suschitzky, Hans
, p. 982 - 994 (2007/10/02)
The title nitrenes, derived by nitro-group deoxygenation with triethyl phosphite or by thermolysis or photolysis of the corresponding azide, have been studied.The effect of substituents (Cl, Br, OMe, NMe2, Me, CF3, and NO2) both meta and para to the nitrene has been examined as a determinant of the preferred mode of cyclisation to either a pyrazolobenzotriazole or a pyrazoloquinoxaline.Similarly, the role of solvents, sensitisers, and quenchers has been studied.Routes to the isomeric 1- and 2-(2-nitrophenyl)-4,5,6,7-tetrahydroindazoles have been defined and the literature corrected by studing the nitrene-mediated cyclisation of these products.The chemistry of the analogous 1-(2-carbenophenyl)- and the 1-(2-nitrenosulphonylphenyl)-3,5-dimethylpyrazoles has also been examined, the former giving 2-(3,5-dimethylpyrazol-1-yl)-benzaldazine and -benzyl alcohol while the latter gave products of intramolecular nitrene attack (a pyrazolobenzothiatriazine) and intermolecular reaction.Rationalisations for all the reaction pathways have been advanced.
