82882-56-2Relevant academic research and scientific papers
Synthesis, characterization and dynamic behavior of (π-allyl)palladium complexes with polydentate nitrogen ligands, evidence of a dissociative mechanism
Elguero, Jose,Fruchier, Alain,De La Hoz, Antonio,Jalon, Felix A.,Manzao, Blanca R.,Oteroo, Antonio,Torre, Felipe Gomez-De La
, p. 589 - 594 (1996)
New examples of the fluxional behavior of (η3-allyl)palladium complexes are described. Variable-temperature experiments and line-shape analysis of two (η3-allyl)palladium complexes containing 2-(1H-pyrazol-1-yl)azine ligands were performed in order to determine the activation free energies, enthalpies and entropies of the process. A dissociative mechanism pointing to a selective Pd-N cleavage is proposed on the basis of these results and NOE experiments above and below the coalescence temperature. VCH Verlagsgesellschaft mbH, 1996.
A four-coordinate Cu(I)–N-heterocyclic carbene complex: Synthesis, structure, properties, and application in amination for the synthesis of 1-(2-N-heteroaryl)-1H-pyrazoles
Xu, Chen,Li, Hong-Mei,Wang, Zhi-Qiang,Fu, Wei-Jun
, p. 689 - 694 (2020/06/01)
A new luminescent, cationic, heteroleptic, four-coordinate Cu(I)–N-heterocyclic carbene complex [Cu(Br-Pyim)(POP)](PF6) is successfully prepared and characterized, where Br-Pyim and POP are 1-(6-bromopyridin-2-yl)imidazole-3-benzyl-2-ylidene an
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 1477, (2018/04/17)
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column, (2015/03/31)
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 111, (2013/07/31)
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues
Large, Jonathan M.,Osborne, Simon A.,Smiljanic-Hurley, Ela,Ansell, Keith H.,Jones, Hayley M.,Taylor, Debra L.,Clough, Barbara,Green, Judith L.,Holder, Anthony A.
, p. 6019 - 6024 (2013/10/22)
The structural diversity and SAR in a series of imidazopyridazine inhibitors of Plasmodium falciparum calcium dependent protein kinase 1 (PfCDPK1) has been explored and extended. The opportunity to further improve key ADME parameters by means of lowering log D was identified, and this was achieved by replacement of a six-membered (hetero)aromatic linker with a pyrazole. A short SAR study has delivered key examples with useful in vitro activity and ADME profiles, good selectivity against a human kinase panel and improved levels of lipophilic ligand efficiency. These new analogues thus provide a credible additional route to further development of the series.
Synthesis, X-ray characterization and computational Studies of N-imidazolyl and N-pyrazolyl pyrimidine derivatives
Torres, Marta,Ca?ellas, Pablo,Estarellas, Carolina,García-Raso, Angel,Fiol, Juan J.,Albertí, Francisca M.,Frontera, Antonio,Molins, Elies,Mata, Ignasi,Deyà, Pere M.
experimental part, p. 2374 - 2382 (2012/04/17)
In this manuscript we report the synthesis and X-ray characterization of neutral 2-(1H-imidazol-1-yl)-pyrimidine (1), 2-(1H-pyrazol-1-yl)-pyrimidine (2) and 1-(2-pyrimidinyl)-1H-benzimidazole (3). We have also obtained crystals of the corresponding hydrochlorides of compounds 1 and 3. Finally, the outer sphere complex of protonated 2-(1H-imidazol-1-yl)-pyrimidine with [CoCl 4]2- as counterion is described. In several charged structures interesting anion-π interactions determine the crystal packing. Moreover, in neutral systems some stacking interactions are governed by double lone pair-π interactions. High level ab initio calculations (RI-MP2/def2-TZVP) have been used to evaluate the noncovalent interactions observed in the solid state and the interplay between them.
N-aryl pyrazoles: DFT calculations of CH acidity and deprotonative metallation using a combination of lithium and zinc amides
Chevallier, Floris,Halauko, Yury S.,Pecceu, Christelle,Nassar, Ibrahim F.,Dam, To Uyen,Roisnel, Thierry,Matulis, Vadim E.,Ivashkevich, Oleg A.,Mongin, Florence
scheme or table, p. 4671 - 4684 (2011/07/07)
A series of N-aryl and N-heteroaryl pyrazoles have been deproto-metallated using a 2,2,6,6-tetramethylpiperidino-based mixed lithium-zinc combination. Mono-, di-, and tri-iodides have been obtained after subsequent trapping with iodine, depending on the s
Direct, metal-free amination of heterocyclic amides/ureas with NH-heterocycles and N-substituted anilines in POCl3
Deng, Xiaohu,Roessler, Armin,Brdar, Ivana,Faessler, Roger,Wu, Jiejun,Sales, Zachary S.,Mani, Neelakandha S.
experimental part, p. 8262 - 8269 (2011/12/04)
A POCl3-mediated, direct amination reaction of heterocyclic amides/ureas with NH-heterocycles or N-substituted anilines is described. Compared to the existing methods, this operationally simple protocol provides unique reactivity and functional
HETEROCYCLIC COMPOUNDS AND USE THEREOF AS ERK INHIBITORS
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Page/Page column 252, (2009/01/23)
Disclosed are the ERK inhibitors of formula 1.0: [Formula (1.0)] and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
