Zhang, Dawei et al. published their patent in 2015 |CAS: 16230-24-3

The Article related to pyrimidine preparation egfr t790m kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 16230-24-3

On August 13, 2015, Zhang, Dawei published a patent.Application of 16230-24-3 The title of the patent was Substituted pyrimidines useful as EGFR-T790M kinase inhibitors and their preparation. And the patent contained the following:

The invention is directed to pyrimidines of formula I, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases and/or mutants mediated diseases and conditions. Compounds of formula I wherein R1 is H, C1-6 alkoxy, F, Cl and CF3; R2 is C1-6 alkyl and acyl; with provisions; and pharmaceutically acceptable salts, solvates, prodrugs, stereoisomers, tautomers and metabolites thereof, are claimed. Example compound II was prepared by amination of 2,4-dichloro-5-(trifluoromethyl)pyrimidine with 1-(4-(4-aminophenyl)piperazin-1-yl)ethanone; the resulting 1-[4-[4-[[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone underwent amination with N-(3-aminophenyl) prop-2-enamide to give compound II. The invention compounds were evaluated for their EGFR-T790M kinase inhibitory activity. From the assay, it was determined that compound II exhibited Kd value of 0.54 nM. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to pyrimidine preparation egfr t790m kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics