306745-64-2Relevant academic research and scientific papers
Diamine Synthesis via the Nitrogen-Directed Azidation of σ- And π-C-C Bonds
Nguyen, Tin V. T.,Wang, Ming-Ming,Waser, Jerome
supporting information, p. 11969 - 11975 (2021/08/24)
Diamines are essential building blocks for the synthesis of agrochemicals, drugs, and organic materials, yet their synthesis remains challenging, as both nitrogens need to be differentiated and diverse substitution patterns (1,2, 1,3, or 1,4) are required. We report herein a new strategy giving access to 1,2, 1,3, and 1,4 amido azides as orthogonally protected diamines based on the nitrogen-directed diazidation of alkenes, cyclopropanes, and cyclobutanes. Commercially available copper thiophene-2-carboxylate (CuTc, 2 mol %) as catalyst promoted the diazidation of both πand σ C-C bonds within 10 min in the presence of readily available oxidants and trimethylsilyl azide. Selective substitution of the formed α-amino azide by carbon nucleophiles (electron-rich aromatic, malonate, organosilicon, organoboron, organozinc, and organomagnesium compounds) was then achieved in a one-pot fashion, leading to the formation of 1,2-, 1,3-, and 1,4-diamines with the amino groups protected orthogonally as an amide/carbamate and an azide.
Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases
Muth, Felix,Günther, Marcel,Bauer, Silke M.,D?ring, Eva,Fischer, Sabine,Maier, Julia,Drückes, Peter,K?ppler, Jürgen,Trappe, J?rg,Rothbauer, Ulrich,Koch, Pierre,Laufer, Stefan A.
supporting information, p. 443 - 456 (2015/07/27)
Tetra-substituted imidazoles were designed as dual inhibitors of c-Jun N-terminal kinase (JNK) 3 and p38α mitogen-activated protein (MAP) kinase. A library of 45 derivatives was prepared and evaluated in a kinase activity assay for their ability to inhibi
ANTI-VIRAL COMPOUNDS
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Page/Page column 54, (2008/12/06)
Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flavivi
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors
Jones, Clifford D.,Andrews, David M.,Barker, Andrew J.,Blades, Kevin,Byth, Kate F.,Finlay, M. Raymond V.,Geh, Catherine,Green, Clive P.,Johannsen, Marie,Walker, Mike,Weir, Hazel M.
body text, p. 6486 - 6489 (2009/10/01)
The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. The series was found to have much improved CDK2 inhibition and potent in vitro anti-proliferative effects against cancer cell lines. Control of overall lipophilicity was important to achieve good in vitro potency along with acceptable physiochemical properties and margins against inhibition of both CYP isoforms and the hERG potassium ion channel. A compound with an attractive overall balance of properties was profiled in vivo and possessed suitable physiochemical and pharmacokinetic profiles for oral dosing.
N-(6-MEMBERED AROMATIC RING)-AMIDO ANTI-VIRAL COMPOUNDS
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Page/Page column 91, (2008/06/13)
Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.
4- (4- (IMIDAZOL-4-YL) PYRIMIDIN-2-YLAMINO) BENZAMIDES AS CDK INHIBITORS
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Page/Page column 61, (2008/06/13)
Compounds of the formula: (I): wherein variable groups are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
