305811-46-5Relevant academic research and scientific papers
A simple synthesis of 5-(2-Aminophenyl)-1H-pyrazoles
Janjic, Monika,Prebil, Rok,Groselj, Uros,Kralj, David,Malavasic, Crt,Golobic, Amalija,Stare, Katarina,Dahmann, Georg,Stanovnik, Branko,Svete, Jurij
experimental part, p. 1703 - 1717 (2011/10/31)
A four-step synthesis of 1-substituted 5-(2-aminophenyl)-1H-pyrazoles 5 as a novel type of histamine analogs and versatile building blocks for further transformations was developed. The synthesis starts from commercially available 2-nitroacetophenone (12), which is converted into the enamino ketone 13 as the key intermediate. Cyclization of the key intermediate 13 with monosubstituted hydrazines 14a-14l afforded the 5-(2-nitrophenyl)-1H-pyrazoles 17a-17l. Finally, catalytic hydrogenation of the nitro compounds 17a, 17c-17e, and 17g-17j furnished the title compounds 5a, 5c-5e, and 5g-5j, respectively, in good yields. As demonstrated by some further transformations, additional functionalization of compounds 17 and 5 is feasible, either by electrophilic substitution at C(4) of the pyrazole ring, or at the NH2 group. Copyright
Pyrazole compounds
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Page/Page column 82, (2008/06/13)
Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination wit
Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Page/Page column 36-37, (2010/02/11)
Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.
2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: α1a subtype selective 2′-heteroaryl compounds
Speake, Jason D.,Navas III, Frank,Bishop, Michael J.,Garrison, Deanna T.,Bigham, Eric C.,Hodson, Stephen J.,Saussy, David L.,Liacos, Jim A.,Irving, Paul E.,Sherman, Bryan W.
, p. 1183 - 1186 (2007/10/03)
The structure-activity relationship of 2′-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as α1 adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent α1A subtype selective agonists have been identified.
