72954-83-7Relevant articles and documents
Beyond the five and six: Evaluation of seven-membered cyclic anhydrides in the castagnoli-cushman reaction
Adamovskyi, Mykhailo I.,Ryabukhin, Sergey V.,Sibgatulin, Dmitriy A.,Rusanov, Eduard,Grygorenko, Oleksandr O.
supporting information, p. 130 - 133 (2017/09/08)
The Castagnoli-Cushman reaction with benzo[d]- oxepine-2,4(1H,5H)-dione as an anhydride component allowed for preparation of 2,3-disubstituted 4-oxo-2,3,4,5-tetrahydro-1H-benzo[d]- azepine-1-carboxylic acids in 21-75% yields and with good trans diastereoselectivity. The method worked with imines generated from aromatic or a-branched aliphatic aldehydes and is amenable for both parallel synthesis and scale-up. The procedure for epimerization of the resulting trans-disubstituted tetrahydrobenzo[d]azepines to their cis isomers was also developed.
Structural-activity relationship study of highly-functionalized imidazolines as potent inhibitors of nuclear transcription factor-κB mediated IL-6 production
Kahlon, Daljinder K.,Lansdell, Theresa A.,Fisk, Jason S.,Tepe, Jetze J.
experimental part, p. 3093 - 3103 (2009/10/02)
We herein describe the synthesis and anti-inflammatory properties of a small library of imidazoline-based NF-κB inhibitors. The structure-activity relationship of various substituents on an imidazoline core structure was evaluated for the ability to inhibit NF-κB mediated IL-6 production. Optimization of the scaffolds was pursued by correlating luciferase-based NF-κB reporter assays with inhibition of IL-6 production in IL-1β stimulated human blood. Several derivatives were found to inhibit NF-κB mediated IL-6 production in the nanomolar range in IL-1β stimulated human blood.
Aminophosphinic acids in a pyridine series: Cleavage of pyridine-2- and pyridine-4-methyl(amino)phosphinic acids in acidic solutions
Boduszek, Bogdan,Olszewski, Tomasz,Goldeman, Waldemar,Konieczna, Magdalena
, p. 787 - 795 (2007/10/03)
The synthesis of a series of new pyridine aminomethylphosphinic acids is described. These compounds were obtained in the reaction of the corresponding pyridine aldehydes with primary amines and with ethyl phenylphosphinate, or methylphosphinate, in the presence of bromotrimethylsilane. In aqueous, strong acid solutions, pyridine aminophosphinic acids were split, forming the phenyl-, or methylphosphonic, acid and the corresponding secondary pyridyl-alkylamines. The kinetics of some observed cleavages were measured, and a mechanism of the cleavage has been proposed. Copyright Taylor & Francis Group, LLC.