2915-15-3Relevant articles and documents
Microwave-assisted synthesis of phenylpyrimidine derivatives via Suzuki-Miyaura reactions in water
Le, Yi,Zhang, Yan,Wang, Qin,Rao, Nian,Li, Dan,Liu, Li,Ouyang, Guiping,Yan, Longjia
supporting information, (2021/02/21)
An efficient method was developed to prepare biphenylpyrimidine scaffolds via a Suzuki-Miyaura coupling reaction. In this procedure, the products were synthesized under microwave irradiation in water and analogues of biguanidine were employed as ligands.
Pyrimidine as an Aryl C-H Activating Group
Gupta, Sahaj,Melanson, Jennifer A.,Vaillancourt, Louis,Nugent, William A.,Tanoury, Gerald J.,Schatte, Gabriele,Snieckus, Victor
supporting information, p. 3745 - 3748 (2018/07/22)
The Pd-catalyzed regioselective C-H activation/arylation, /iodination, and/acetoxylation reactions of 4-arylpyrimidines using aryl iodides, N-iodosuccinimide, and (diacetoxyiodo)benzene respectively as coupling partners are described. Suzuki-Miyaura coupl
Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead
Mologni, Luca,Dalla Via, Martina,Chilin, Adriana,Palumbo, Manlio,Marzaro, Giovanni
, p. 1390 - 1398 (2017/09/01)
Oncogenic activation of RET kinase has been found in several neoplastic diseases, like medullary thyroid carcinoma, multiple endocrine neoplasia, papillary thyroid carcinoma, and non-small-cell lung cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Hence, novel compounds able to inhibit both wild-type RET (wtRET) and its mutants (e.g., V804MRET) are needed. Herein we present the development and the preliminary evaluation of a new sub-micromolar wtRET/V804MRET inhibitor, N-(2-fluoro-5-trifluoromethylphenyl)-N′-{4′-[(2′′-benzamido)pyridin-4′′-ylamino]phenyl}urea (69), endowed with a 4-anilinopyridine structure, starting from our previously identified 4-anilinopyrimidine hit compound. Profiling against a panel of kinases indicated 69 as a multi cKIT/wtRET/V804MRET inhibitor.