1263319-52-3Relevant academic research and scientific papers
A tandem amination/lactamisation route to 2-Azabicyclo[2.2.2]octanones
Cuthbertson, James D.,Godfrey, Andrew A.,Taylor, Richard J. K.
, p. 2805 - 2807 (2010)
An efficient one-pot amination/lactamisation sequence for the preparation of 2-azabicyclo[2.2.2]octanones from 6-carboalkoxycyclohex-2-enones and aqueous ammonia is described. Scope and limitation studies are reported for this tandem procedure and a range of bicyclic compounds have been prepared, two of which were characterised by X-ray crystallography.
Hypervalent-Iodine-Mediated Formation of Epoxides from Carbon(sp2)-Carbon(sp3) Single Bonds
Jiang, Shan,Yan, Tai-Shan,Han, Yong-Chao,Cui, Li-Qian,Xue, Xiao-Song,Zhang, Chi
, p. 11691 - 11702 (2017/11/24)
We have developed an efficient method for direct formation of epoxide groups from carbon(sp2)-carbon(sp3) single bonds of β-keto esters; the reaction is mediated by the water-soluble hypervalent iodine(V) reagent AIBX (5-trimethylammonio-1,3-dioxo-1,3-dihydro-1λ5-benzo[d][1,2]iodoxol-1-ol anion). On the basis of the results of density functional theory calculations and experimental studies, we propose that the reaction proceeds by a two-stage mechanism involving dehydrogenation of the β-keto ester substrates and epoxidation of the resulting enone intermediates. The rate-limiting step is abstraction of the β′-C-H (calculated free energy of activation, 24.5 kcal/mol).
Arginase Inhibitors and Their Therapeutic Applications
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Paragraph 0564; 0565; 0566; 0901; 0902; 0903, (2017/11/29)
Disclosed are small molecule therapeutic compounds that are potent inhibitors of arginase 1 and arginase 2 activity. Also disclosed are pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a
