Synthesis and biological research of 2-aryl-4-morpholino-6-triazolylpyrimidine derivatives as antitumor PI3K inhibitors was written by Yang, Xiu-li;Wang, Tian-cai;Lin, Sen;Fan, Hou-xing. And the article was included in Jingxi Huagong in 2014.Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine This article mentions the following:
In order to find more active antitumor PI3K inhibitors, pyrimidine-2,4-diol was used as raw material to go through chlorination by POCl3, coupling with morpholine, then iodine generation, which was followed by Sonogashira coupling to remove the trimethylsilyl in order to get the triazolyl intermediate. Finally, the intermediate went through Suzuki coupling to give 2-aryl-4-morpholino-6-triazolylpyrimidine 14-27. Their structures were confirmed by 1HNMR and LC-MS. The in vitro anti-proliferative activity assay against A2780 was carried out by MTT detection method, and the results showed that, at the test concentration of 10μmol/L, the compounds 14 and 25 were more potent than clin. candidates GDC-0941 and BEZ-235, the inhibition rate of which reached 76.7% and 77.2%, resp. Furthermore, the results of pharmacokinetic study suggested that compound 25 was desirable: t1/2 = 3.2 h, and AUC0-∞ was 34,193 (ng·h)/mL. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine).
4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia