444583-14-6Relevant articles and documents
Simple Aza -conjugate addition methodology for the synthesis of isoindole nitrones and 3,4-dihydroisoquinoline nitrones
Peacock, Lucy R.,Chapman, Robert S. L.,Sedgwick, Adam C.,Bull, Steven D.,Mahon, Mary F.,Amans, Dominique
, p. 994 - 997 (2015/03/18)
Aryl-aldehydes containing ortho-substituted α,β-unsaturated carboxylic acid derivatives react with hydroxylamine to afford reactive N-hydroxy-carbinolamine intermediates that undergo intramolecular aza-conjugate addition reactions to afford isoindole nitrones and 3,4-dihydroisoquinoline nitrones in good yield. Conditions have been developed to reduce these isoindole nitrones to their corresponding hydroxylamine, enamine, and amine derivatives. Isoindole nitrones react with dimethyl acetylenedicarboxylate (DMAD) via a [4 + 2]-cycloaddition/deamination pathway to afford substituted naphthalene derivatives, while 3,4-dihydroisoquinoline nitrones react with DMAD via a [1,3]-dipolar cycloaddition pathway to afford tricyclic heteroarenes.
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor
Shi, Qing,Ornstein, Paul L.,Briner, Karin,Richardson, Timothy I.,Arnold, Macklin B.,Backer, Ryan T.,Buckmaster, Jennifer L.,Canada, Emily J.,Doecke, Christopher W.,Hertel, Larry W.,Honigschmidt, Nick,Hsiung, Hansen M.,Husain, Saba,Kuklish, Steve L.,Martinelli, Michael J.,Mullaney, Jeffrey T.,O'Brien, Thomas P.,Reinhard, Matt R.,Rothhaar, Roger,Shah, Jikesh,Wu, Zhipei,Xie, Chaoyu,Zgombick, John M.,Fisher, Matthew J.
, p. 2341 - 2346 (2007/10/03)
A series of benzylic piperazines (e.g., 4 and 5) attached to an 'address element', the dipeptide H-d-Tic-d-p-Cl-Phe-OH, 3 has been identified as ligands for the melanocortin subtype-4 receptor (MC4R). We describe herein the structure-activity relationship (SAR) studies on the N-terminal residue of the 'address element'. Several novel dipeptides and reduced dipeptides with high MC4R binding affinities and selectivity emerged from this SAR study.
Piperazine- and piperidine-derivatives as melanocortin receptor agonists
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Page/Page column 95, (2010/02/06)
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.