13148-43-1Relevant articles and documents
A practical one-pot synthesis of 5-aryl-2-furaldehydes
McClure,Roschangar,Hodson,Millar,Osterhout
, p. 1681 - 1685 (2001)
A useful one-pot synthesis of 5-aryl-2-furaldehydes via palladium-mediated Suzuki coupling of aryl halides with in situ generated 5-(diethoxymethyl)-2-furylboronic acid is described. The procedure has general applicability, delivers high yields, and is amenable to scale-up.
5-Aryl-2-furaldehydes in the synthesis of tetrahydropyrimidinones by Biginelli reaction
Vakhula, Andriy R.,Horak, Yuriy I.,Lytvyn, Roman Z.,Lesyuk, Alexandra I.,Kinzhybalo, Vasyl,Zubkov, Fedor I.,Obushak, Mykola D.
, p. 545 - 549 (2018/07/05)
5-Aryl-2-furaldehydes, obtained by furfural arylation with arenediazonium salts, react with ethyl acetoacetate or acetylacetone and (thio)- urea in the presence of FeCl3·6H2O as a catalyst. A series of ethyl 4-(5-aryl-2-furyl)-6-methyl-2-oxo(thioxo)-1,2,3,4-tetrahydropyrimidine- 5-carboxylates was obtained.
2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors
Tiberi, Marika,Tintori, Cristina,Ceresola, Elisa Rita,Fazi, Roberta,Zamperini, Claudio,Calandro, Pierpaolo,Franchi, Luigi,Selvaraj, Manikandan,Botta, Lorenzo,Sampaolo, Michela,Saita, Diego,Ferrarese, Roberto,Clementi, Massimo,Canducci, Filippo,Botta, Maurizio
supporting information, p. 3043 - 3052 (2014/06/09)
We report here the synthesis of 2-Aminothiazolones along with their biological properties as novel anti-HIV agents. Such compounds have proven to act through the inhibition of the gp120-CD4 protein-protein interaction that occurs at the very early stage of the HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains and pseudotyped viruses were documented. Docking simulations have also been applied to predict the mechanism, at the molecular level, by which the inhibitors were able to interact within the Phe43 cavity of HIV-1 gp120. Furthermore, a preliminary absorption, distribution, metabolism, and excretion (ADME) evaluation was performed. Overall, this study led the basis for the development of more potent HIV entry inhibitors.