424800-71-5Relevant articles and documents
Practical synthesis of 3,3-substituted dihydroquinoxalin-2-ones from aryl 1,2-diamines using the Bargellini reaction
Alanine, Thomas A.,Stokes, Stephen,Scott, James S.
, p. 4386 - 4388 (2016)
The reaction of aromatic 1,2-diamines with trichloromethylcarbinols under mild, basic phase-transfer conditions provided expedient access to 3,3-disubsituted quinoxalin-2(1H)-ones in good to moderate yields. The use of unsymmetrical aryl diamines gave a r
QUINOXALINE DERIVATIVES AS MODULATORS OF THE GLUCOCORTICOID RECEPTOR
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Page/Page column 41-42, (2021/07/24)
The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β
Wang, Yikai,Wach, Jean-Yves,Sheehan, Patrick,Zhong, Cheng,Zhan, Chenyang,Harris, Richard,Almo, Steven C.,Bishop, Joshua,Haggarty, Stephen J.,Ramek, Alexander,Berry, Kayla N.,O'Herin, Conor,Koehler, Angela N.,Hung, Alvin W.,Young, Damian W.
supporting information, p. 852 - 856 (2016/10/12)
Traditional fragment-based drug discovery (FBDD) relies heavily on structural analysis of the hits bound to their targets. Herein, we present a complementary approach based on diversity-oriented synthesis (DOS). A DOS-based fragment collection was able to produce initial hit compounds against the target GSK3β, allow the systematic synthesis of related fragment analogues to explore fragment-level structure-activity relationship, and finally lead to the synthesis of a more potent compound.
Palladium-catalyzed synthesis of quinoxaline derivatives
Wallace, Jeffery M.,S?derberg, Bj?rn C.G.,Tamariz, Joaquín,Akhmedov, Novruz G.,Hurley, Mathew T.
, p. 9675 - 9684 (2008/12/22)
A palladium-catalyzed reductive N-heteroannulation of enamines derived from 2-nitrobenzenamines forming mixtures of 1,2-dihydroquinoxalines and 3,4-dihydroquinoxalin-2-ones is described. The reactions are performed using bis(dibenzylideneacetone)palladium(0), 1,3-bis(diphenylphosphino)propane, and 1,10-phenanthroline in DMF under 6 atm of carbon monoxide at 70 °C.
A novel palladium-catalyzed synthesis of 1,2-dihydroquinoxalines and 3,4-dihydroquinoxalinones.
Soederberg, Bjoern C G,Wallace, Jeffery M,Tamariz, Joaquin
, p. 1339 - 1342 (2007/10/03)
Reactions of enamines, derived from 2-nitroanilines and alpha-substituted aldehydes, with carbon monoxide (6 atm) in the presence of a catalytic amount of bis(dibenzylideneacetone)palladium(0) (Pd(dba)(2)) and 1,3-bis(diphenylphosphino)propane (dppp) affo