111562-32-4Relevant articles and documents
Regioselective Synthesis of o-Benzenediboronic Acids via Ir-Catalyzed o-C-H Borylation Directed by a Pyrazolylaniline-Modified Boronyl Group
Yamamoto, Takeshi,Ishibashi, Aoi,Suginome, Michinori
supporting information, p. 886 - 889 (2017/02/26)
Ir-catalyzed ortho-directed C-H borylation of pyrazolylaniline (PZA)-modified arylboronic acids with bis(pinacolate)diboron afforded o-benzenediboronic acids in which two boronyl groups are differentially modified by pinacol (PIN) and PZA. By using this borylation after nondirected Ir-catalyzed C-H borylation, o-benzenediboronic acids are conveniently synthesized from unfunctionalized arenes. The differentially modified o-benzenediboronic acids undergo selective oxidation and Suzuki-Miyaura cross-coupling at the PZA-modified boronyl groups, affording o-functionalized arylboronic acids selectively.
TRIAZOLO- AND PYRAZOLOQUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITOR
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, (2012/02/02)
The invention relates to compounds of the formula (I) and their use as pharmaceutical ingredients, in particular for the treatment of CNS related diseases.
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
, 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
Easily attachable and detachable ortho-directing agent for arylboronic acids in ruthenium-catalyzed aromatic C-H silylation
Ihara, Hideki,Suginome, Michinori
supporting information; experimental part, p. 7502 - 7503 (2009/10/16)
(Chemical Equation Presented) o-C?H silylation of arylboronic acids has been achieved using 2-pyrazol-5-ylaniline as an orthodirecting agent, which was temporarily attached to the boronyl group via Ru-catalyzed silylation with hydrosilanes. Condensation products of arylboronic acids with2-pyrazol-5-ylaniline were prepared in situ and subjected to reaction w ith triorganosilanes in the presence of RuH2(CO)(PPh3) 3 at 135°C. Regioselective silylation at their ortho-positions proceeded in good yields for phenylboronic acids bearing para-substituents such as chloro, fluoro, methyl, methoxy, and trifluoromethyl groups. p-Methoxycarbonyl-substituted phenylboronic acid provided thecorresponding silylated product in moderate yield. m-Tolyl- and 2-napht hylboronic acids underwent silylation selectively at the less stericallyhindered ortho-positions. The silylated products were utilized in Suzuk i?Miyaura coupling, followed either by iodination with ICl or by Tamao oxidation to furnish iodine- or hydroxy-substituted biaryls.
Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Page/Page column 38, (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.
Inhibitors of C-FMS kinase
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, (2008/06/13)
The invention relates to compounds of Formula I: wherein A is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoal
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.
Imidazodiazepine derivatives
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, (2008/06/13)
The novel imidazodiazepine derivatives of the formula: STR1 wherein the substituents are as described in the specification, can be used for the control or prevention of epileptic seizures, anxiety, tension and excitation states, sleep disorders, schizophr
New Tetracyclic Derivatives of Imidazobenzodiazepines and of Imidazothienodiazepines
Gerecke, Max,Kyburz, Emilio,Borer, Rene,Gassner, Walter
, p. 693 - 722 (2007/10/02)
The synthesis of new tetracyclic 1,4-diazepine derivatives is described.In these compounds, an additional five-membered heterocycle is fused on the known tricyclic ring systems imidazobenzodiazepine and imidazothienodiazepine.Many of these new compounds display a very high affinity to the benzodiazepine receptor in mammals.
