15969-46-7Relevant articles and documents
2,4,6-Trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists
Chang, Lisa C. W.,Spanjersberg, Ronald F.,Von Frijtag Drabbe Künzel, Jacobien K.,Mulder-Krieger, Thea,Van Den Hout, Gijs,Beukers, Margot W.,Brussee, Johannes,IJzerman, Adriaan P.
, p. 6529 - 6540 (2004)
Adenosine receptor antagonists usually possess a bi- or tricyclic heteroaromatic structure at their core with varying substitution patterns to achieve selectivity and/or greater affinity. Taking into account molecular modeling results from a series of pot
A phosphine-catalyzed preparation of 4-Arylidene-5-imidazolones
Gabillet, Sandra,Loreau, Olivier,Specklin, Simon,Rasalofonjatovo, Evelia,Taran, Frdric
, p. 9894 - 9898 (2015/01/09)
A simple and efficient method for constructing 4-arylidene-5-imidazolones was developed using a phosphinecatalyzed tandem umpolung addition and intramolecular cyclization of amidine pronucleophiles on arylpropiolates. The reaction offers a robust route to heterocycle analogues of the fluorescent protein chromophores. (Chemical Equation Presented).
A metal-free tandem approach to prepare structurally diverse N-heterocycles: Synthesis of 1,2,4-oxadiazoles and pyrimidinones
Gupta, Puneet K.,Hussain, Mohd. Kamil,Asad, Mohd.,Kant, Ruchir,Mahar, Rohit,Shukla, Sanjeev K.,Hajela, Kanchan
, p. 3062 - 3070 (2014/07/07)
A metal-free one-pot approach to the diversity oriented synthesis of N-heterocycles, 1,2,4-oxadiazoles and 2,6 disubstituted pyrimidin-4-ones is described via carboxamidation of amidines with aryl carboxylic acids and aryl propargylic acids. The reactions occur at room temperature forming N-acylamidines which undergo tandem nucleophilic addition-deamination- intramolecular cyclisation to give the corresponding heterocyclic compounds in good to excellent yields. This one pot approach has led to the successful synthesis of the drug lead molecule, ataluren, 3-(5-(2-fluorophenyl)-1,2,4- oxadiazol-3-yl) benzoic acid in two steps. the Partner Organisations 2014.