449804-01-7Relevant articles and documents
Copper(II)-Catalysed Aerobic Oxidative Coupling of Arylamines with Hexafluoroisopropanol: An Alternative Methodology for Constructing Fluorinated Compounds
Guo, Jiabao,Li, Zhanchong,Song, Yang,Wu, Liangying,Yao, Xiaoquan
supporting information, p. 268 - 274 (2020/12/04)
The selective functionalisation of arylamine derivatives with hexafluoroisopropanol through copper(II)-catalysed aerobic oxidative coupling was developed to generate various fluoroalkylated arylamines under mild conditions. This method has a wide substrat
Cobalt-Catalyzed Selective Functionalization of Aniline Derivatives with Hexafluoroisopropanol
Zhao, He,Zhao, Shuo,Li, Xiu,Deng, Yinyue,Jiang, Huanfeng,Zhang, Min
supporting information, p. 218 - 222 (2019/01/10)
A cobalt-catalyzed site-selective functionalization of aniline derivatives with hexafluoroisopropanol, which enables the synthesis of a wide array of fluoroalkylated anilines, a class of highly valuable building blocks for further preparation of fluorinated functional products, is reported. The developed transformation proceeds with operational simplicity, use of earth-abundant metal catalyst, broad substrate scope, good functional group tolerance, and mild reaction conditions.
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand
Nishiyama, Yuko,Nakamura, Masahiko,Misawa, Takashi,Nakagomi, Madoka,Makishima, Makoto,Ishikawa, Minoru,Hashimoto, Yuichi
, p. 2799 - 2808 (2014/05/06)
Retinoic acid receptor-related orphan receptors (RORs), which belong to the nuclear receptor superfamily, regulate many physiological processes, including hepatic gluconeogenesis, lipid metabolism, immune function and circadian rhythm. Since RORs resemble liver X receptors (LXRs) in the fold structure of their ligand-binding domains, we speculated that ROR-mediated transcription might be modulated by LXR ligands, in line with the multi-template hypothesis. Therefore, we screened our LXR ligand library for compounds with ROR ligand activity and identified a novel ROR ligand with a phenanthridin-6(5H)-one skeleton. Structure-activity relationship studies aimed at separating ROR inverse agonistic activity from LXR-agonistic activity enabled us to develop a series of ROR inverse agonists based on the phenanthridin-6(5H)-one skeleton, including a RORγ-selective inverse agonist.
Structure-guided design of N-phenyl tertiary amines as transrepression- selective liver X receptor modulators with anti-inflammatory activity
Chao, Esther Y.,Caravella, Justin A.,Watson, Mike A.,Campobasso, Nino,Ghisletti, Serena,Billin, Andrew N.,Galardi, Cristin,Wang, Ping,Laffitte, Bryan A.,Iannone, Marie A.,Goodwin, Bryan J.,Nichols, Jason A.,Parks, Derek J.,Stewart, Eugene,Wiethe, Robert W.,Williams, Shawn P.,Smallwood, Angela,Pearce, Kenneth H.,Glass, Christopher K.,Willson, Timothy M.,Zuercher, William J.,Collins, Jon L.
experimental part, p. 5758 - 5765 (2009/10/01)
A cocrystal structure of T1317 (3) bound to hLXRβ was utilized in the design of a series of substituted N-phenyl tertiary amines. Profiling in binding and functional assays led to the identification of LXR modulator GSK9772 (20) as a high-affinity LXRβ li
