1126-44-9Relevant articles and documents
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.
supporting information, 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.
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-α production
Clark, Michael P.,Laughlin, Steven K.,Laufersweiler, Matthew J.,Bookland, Roger G.,Brugel, Todd A.,Golebiowski, Adam,Sabat, Mark P.,Townes, Jennifer A.,VanRens, John C.,Djung, Jane F.,Natchus, Michael G.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Walter, Rick L.,Mekel, Marlene J.,Heitmeyer, Sandra A.,Brown, Kimberly K.,Juergens, Karen,Taiwo, Yetunde O.,Janusz, Michael J.
, p. 2724 - 2727 (2007/10/03)
2-Aryl-3-pyrimidinyl based tumor necrosis factor-α (TNF-α) inhibitors, which contain a novel bicyclic pyrazolone core, are described. Many showed low-nanomolar activity against lipopolysaccharide-induced TNF-α production in monocytic cells. Secondary scre
Synthesis of Pyrimidin-2-one Nucleosides as Acid-Stable Inhibitors of Cytidine Deaminase
Kim, Chong-Ho,Marquez, Victor E.,Mao, David T.,Haines, David R.,McCormack, John J.
, p. 1374 - 1380 (2007/10/02)
One of the problems encountered in the use of the tetrahydrouridine (THU, 2) and saturated 2-oxo-1,3-diazepine nucleosides as orally administered cytidine deaminase (CDA) inhibitors is their acid instability.Under acid conditions these compounds are rapid
