24513-05-1Relevant academic research and scientific papers
Visible-Light-Mediated Synthesis of Pyrazines from Vinyl Azides Utilizing a Photocascade Process
Hossain, Asik,Pagire, Santosh K.,Reiser, Oliver
supporting information, p. 1707 - 1714 (2017/11/27)
A convenient method for the synthesis of substituted pyrazines from vinyl azides has been developed. This method is enabled by a dual-energy and electron-transfer strategy by visible-light photocatalysis. Initially, vinyl azides are activated by a triplet sensitization process from an excited ruthenium photocatalyst in the presence of water to form dihydropyrazines, followed by a single-electron-transfer (SET) process under oxygen (air) atmosphere that leads to the tetrasubstituted pyrazines in good to excellent yields.
Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives
Wang, Rui,Shi, Hong-Fan,Zhao, Jing-Feng,He, Yan-Ping,Zhang, Hong-Bin,Liu, Jian-Ping
supporting information, p. 1760 - 1762 (2013/04/10)
A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and any bulky group should be avoided in order to keep a relative small volume for this kind of molecules.
A novel synthesis of α-azidocinnamates, α-azido-α,β-unsaturated ketones and β-azidostyrenes mediated by cerium(IV) ammonium nitrate
Nair, Vijay,George, Tesmol G.
, p. 3199 - 3201 (2007/10/03)
Cerium(IV) ammonium nitrate mediated addition of azide to cinnamic esters, acids and α,β-unsaturated ketones, followed by reaction with sodium acetate afforded the α-azidocinnamates, β-azidostyrenes and α-azido-α,β- unsaturated ketones, respectively, in good yields. (C) 2000 Elsevier Science Ltd.
Synthetic utility of tert-butyl azidoacetate on the Hemetsberger-Knittel reaction (synthetic studies of indoles and related compounds part 47)
Kondo, Kazuhiro,Morohoshi, Sachiko,Mitsuhashi, Masaharu,Murakami, Yasuoki
, p. 1227 - 1231 (2007/10/03)
The synthetic utility of tert-butyl azidoacetate (7) on the Hemetsberger-Knittel reaction is described. The following two findings are disclosed by using tert-butyl azidoacetate (7): i) in the first step for the synthesis of ethyl indole-2-carboxylate 4,
Novel Indole-2-carboxylates as Ligands for the Strychnine-Insensitive N-Methyl-D-aspartate-Linked Glycine Receptor
Gray, Nancy M.,Dappen, Michael S.,Cheng, Brian K.,Cordi, Alexis A.,Biesterfeldt, John P.,et al.
, p. 1283 - 1292 (2007/10/02)
A series of indole-2-carboxylates were prepared and evaluated for their ability to inhibit the binding at the strychnine-insensitive glycine receptor that is associated with the NMDA-PCP-glycine receptor complex.All of the compounds were selective for the glycine site relative to other sites on the receptor macrocomplex and several of the compounds in this series were found to have submicromolar affinity for this receptor.The lead compound, 2-carboxy-6-chloro-3-indoleacetic acid (Ki = 1.6 μM vsglycine), was also found to noncompetitively inhibit the binding of MK-801, a ligand for the phencyclidine site on the receptor macrocomplex.These latter data suggest that the compound functions as an antagonist at the strychnine-insensitive glycine receptor.The structural activity relationships within this series of indole-2-carboxylates is discussed and several key pharmacophores are identified for this series of glycine ligands.In general, the most potent compounds were the C-3 acetamides, with N-propyl-2-carboxy-6-chloro-3-indoleacetamide having the highest receptor affinity.
