1289555-51-6Relevant articles and documents
Sequential palladium-catalysed direct arylation followed by suzuki coupling of bromo-2-chloropyridines: Simple access to a variety of 2-arylpyridines
Baloch, Marya,Roy, David,Bensaid, Souhila,Guerchais, Veronique,Doucet, Henri
, p. 4454 - 4462,9 (2012)
2-Arylpyridines are an important class of ligands for the synthesis of complexes with physical properties. We observed that the use of 3-, 4- or 5-bromo-2-chloropyridines allows the synthesis of a wide variety of heteroarylated 2-arylpyridines by means of successive direct arylation and Suzuki coupling. For these two reactions, an air-stable catalyst associated to a cheap and nontoxic base was employed as the catalyst. Moreover, a wide range of heteroarenes and functionalised arylboronic acids could be tolerated. Copyright
Palladium-catalyzed c-4 selective coupling of 2,4-dichloropyridines and synthesis of pyridine-based dyes for live-cell imaging
Chen, Jing,Ding, Yechun,He, Chen,Hu, Xin,Huang, Qitong,Kuang, Ying,Liu, Jinbiao,Yang, Min
, p. 6498 - 6508 (2020/06/09)
An alternative process of Pd-catalyzed C-4 selective coupling of 2,4-dichloropyridines with boronic esters was developed, which afforded 24 examples of C-4 coupled pyridines in moderate to good yields. After further arylation, 21 examples of C-2, C-4 diarylated pyridines with a significant photophysical property were obtained, which were applied as pyridine-based dyes into live-cell imaging with good biocompatibility and low toxicity.
Synthesis and structure-activity relationship analysis of 5-HT7 receptor antagonists: Piperazin-1-yl substituted unfused heterobiaryls
Strekowski, Lucjan,Saczewski, Jaros?aw,Raux, Elizabeth A.,Fernando, Nilmi T.,Klenc, Jeff,Paranjpe, Shirish,Raszkiewicz, Aldona,Blake, Ava L.,Ehalt, Adam J.,Barnes, Samuel,Baranowski, Timothy C.,Sullivan, Shannon M.,Sata?a, Grzegorz,Bojarski, Andrzej J.
, (2016/05/24)
A series of piperazin-1-yl substituted unfused heterobiaryls was synthesized as ligands of the 5-HT7 receptors. The goal of this project was to elucidate the structural features that affect the 5-HT7 binding affinity of this class of compounds represented by the model ligand 4-(3-furyl)-2-(4-methylpiperazin-1-yl)pyrimidine (2). The SAR studies included systematical structural changes of the pyrimidine core moiety in 2 to quinazoline, pyridine and benzene, changes of the 3-furyl group to other heteroaryl substituents, the presence of various analogs of the 4-methylpiperazin-1-yl group, as well as additional substitutions at positions 5 and 6 of the pyrimidine. Substitution of position 6 of the pyrimidine in the model ligand with an alkyl group results in a substantial increase of the binding affinity (note a change in position numbers due to the nomenclature rules). It was also demonstrated that 4-(3-furyl) moiety is crucial for the 5-HT7 binding affinity of the substituted pyrimidines, although, the pyrimidine core can be replaced with a pyridine ring without a dramatic loss of the binding affinity. The selected ethylpyrimidine (12) and butylpyrimidine (13) analogs of high 5-HT7 binding affinity showed antagonistic properties in cAMP functional test and varied selectivity profile-compound 12 can be regarded as a dual 5-HT7 /5-HT2A R ligand, and 13 as a multi-receptor (5-HT7 , 5-HT2A , 5-HT6 and D2 ) agent.
Copper-catalyzed Hiyama coupling of (hetero)aryltriethoxysilanes with (hetero)aryl iodides
Gurung, Santosh K.,Thapa, Surendra,Vangala, Adarsh S.,Giri, Ramesh
supporting information, p. 5378 - 5381 (2013/11/06)
A CuI-catalyzed Hiyama coupling was achieved, which proceeds in the absence of an ancillary ligand for aryl-heteroaryl and heteroaryl-heteroaryl couplings. A P,N-ligand is required to obtain the best product yields for aryl-aryl couplings. In addition to facilitating transmetalation, CsF is also found to function as a stabilizer of the [CuAr] species, potentially generated as an intermediate after transmetalation of aryltriethoxysilanes with Cu I-catalysts in the absence of ancillary ligands.
Pyrrolopyrazine Kinase Inhibitors
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Page/Page column 98, (2011/10/10)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
NEW IMAGING AGENTS AND THEIR USE FOR THE DIAGNOSTIC IN VIVO OF NEURODEGENERATIVE DISEASES, NOTABLY ALZHEIMER'S DISEASE AND DERIVATIVE DISEASES
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Page/Page column 43, (2011/05/05)
The present invention relates to new imaging agents and their use for the in vivo diagnostic of neurodegenerative diseases, notably Alzheimer's disease and related diseases.
