On April 5, 2017, Ma, Dawei; Yu, Qiang; Yuan, Junying; Xia, Hongguang; Cai, Dongpo; Wang, Kailiang; Zhang, Chen; Xia, Shanghua published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was 2,4-Diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives as EGFR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:
The invention provides EGFR kinase inhibitor and its preparation method and application.Specifically, the invention provides a compound shown in formula (I), wherein the definition of each group is as noted in the instruction book.Described compound is the effective EGFR inhibitor. The invention provides 2,4-diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives of formula I as EGFR kinase inhibitors and the preparation method and use thereof. Compounds of formula I wherein X and Y are independently N, CH; provided that X and Y are not CH at the same time; R is (un)substituted 5- to 7-membered heterocyclic ring, -NH-(un)substituted 5- to 7-membered heterocyclic ring, etc.; and their preparation method, as well as their use as EGFR kinase inhibitors in the treatment of cancer thereof, are claimed. Compounds of formula I were prepared by using condensation and deacylation as the key steps. All the invention compounds were evaluated for their EGFR inhibitory activity. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide
The Article related to trifluoromethyl pyridine diaminobenzene acrylamide preparation egfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics