916056-77-4Relevant academic research and scientific papers
Reaction of β-alkoxyvinyl α-ketoesters with acyclic NCN binucleophiles – Scalable approach to novel functionalized pyrimidines
Stepaniuk, Oleksandr O.,Rudenko, Tymofii V.,Vashchenko, Bohdan V.,Matvienko, Vitalii O.,Kondratov, Ivan S.,Tolmachev, Andrey A.,Grygorenko, Oleksandr O.
, p. 3472 - 3478 (2019/05/17)
Two protocols for synthesis of series of low-molecular-weight di- and tri-substituted pyrimidines bearing a functional group at the 4th position, which rely on a base-mediated condensation of amidines or guanidines with β-alkoxyvinyl α-keto esters, have been developed. This approach allowed for multigram preparation of novel pyrimidine-4-carboxylates in 21–90% yield. The synthetic utility of these compounds was demonstrated by some standard functional group transformations providing promising building blocks for organic synthesis and drug discovery.
Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines
Moszczyński-P?tkowski, Rafa?,Majer, Jakub,Borkowska, Ma?gorzata,Bojarski, ?ukasz,Janowska, Sylwia,Mat?oka, Miko?aj,Stefaniak, Filip,Smuga, Damian,Bazyd?o, Katarzyna,Dubiel, Krzysztof,Wieczorek, Maciej
, p. 96 - 116 (2018/06/06)
New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.
