244610-62-6Relevant articles and documents
Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand
Colotta, Vittoria,Catarzi, Daniela,Varano, Flavia,Filacchioni, Guido,Cecchi, Lucia,Galli, Alessandro,Costagli, Chiara
, p. 2915 - 2921 (1996)
The synthesis and binding activity at the benzodiazepine receptor of some 2-substituted pyrazolo[1,5-c]quinazolines are reported. The structure- activity relationships and in vitro efficacy of the title compounds, which are devoid of the proton acceptor atom at position 1, are similar to those of some previously reported tricyclic heteroaromatic compounds. This suggests that a proton acceptor at position 1 is an optional binding site of a benzodiazepine receptor ligand which only affects potency.
Synthesis of 2-(1h-indol-2-yl)acetamides via br?nsted acid-assisted cyclization cascade
Aksenov, Alexander V.,Aksenov, Dmitrii A.,Aksenov, Nicolai A.,Griaznov, Georgii D.,Prityko, Lidiya A.,Rubin, Michael,Skomorokhov, Anton A.
, p. 12128 - 12146 (2020/11/10)
An efficient and straightforward Br?nsted-acid mediated cascade process was developed, involving cyclization of readily available β-ketonitriles into 2-aminofurans, and their subsequent recyclization into 2-(1H-indol-2-yl)acetamides is developed. This synthetic route opens a new avenue for an expeditious assembly of various isotryptamine derivatives for medicinal chemistry.
(±)-2-Aryl-2,3-dihydro-4(1H)-quinolinones by a tandem reduction-Michael addition reaction
Bunce, Richard A.,Nammalwar, Baskar
experimental part, p. 613 - 619 (2011/07/31)
An efficient synthesis of (±)-2-aryl-2,3-dihydro-4(1H)-quinolinones has been developed from chalcones prepared from 2′-nitroacetophenone and a series of substituted benzaldehydes. The cyclization sequence is initiated by reduction of the nitro group under dissolving metal conditions using iron powder in concentrated hydrochloric acid. Milder conditions, using acetic acid or acetic acid-phosphoric acid as the reaction medium, were less satisfactory. Procedural details as well as a mechanistic discussion and reaction optimization studies are presented.