21575-13-3Relevant articles and documents
Synthetic method of erlotinib intermediate
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Paragraph 0018; 0029-0038; 0047-0048, (2020/05/29)
The invention relates to a synthesis method of an erlotinib intermediate, which comprises the following steps: reacting 2-bromo-4,5-dimethoxybenzonitrile with formamidine hydrochloride under the actions of alkali and a catalyst to generate a compound 3; reacting with 1-bromo-triethynylbenzene under the catalysis of alkali to generate a compound 2; carrying out a reaction on the compound 2 with 48%hydrobromic acid under the action of a catalyst to obtain a compound 1. The method is mild in condition, simple in step, safe, environmentally friendly and suitable for industrial production.
Discovery and Optimization of 1-(4-chloro-3-(trifluoromethyl)-phenyl)-3-(2-(amino)pyridin-3-yl)ureas as Novel KDR Kinase Inhibitors
Jiao, Yu,Huang, Fei,Xu, Pengfei,Zhang, Yanmin,Yang, Shangyan,Zhang, Danfeng,Lu, Tao,Tang, Weifang
, p. 328 - 337 (2016/10/12)
Kinase insert Domain-containing Receptor (KDR) is one of the currently validated targets for anticancer drug discovery and development. Herein, a series of o-amino-arylurea derivatives have been synthesized and evaluated for their kinase inhibitory activity. The optimization on the basis of biological screening and molecular modeling resulted in obvious increase in KDR kinase inhibitory activity compared with the hit compound. Eventually, we identified a potent inhibitor 5a of 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-((quinolin-4-ylmethyl) amino)pyridin-3-yl)urea scaffold against KDR (IC50 = 0.0689 μM), which can serve as good starting point for further KDR inhibitor optimization and development.
Polycyclic N-heterocyclic compounds, part 67: Reaction of 6,7-substituted N-(quinazolin-4-yl)amidine derivatives with hydroxylamine hydrochloride: Formation of in vitro inhibitors of pentosidine
Okuda, Kensuke,Muroyama, Hideki,Hirota, Takashi
experimental part, p. 1407 - 1413 (2012/01/05)
Reactions of N-(quinazolin-4-yl)amidines and their amide oximes with hydroxylamine hydrochloride gave cyclization products that were formed by an initial ring cleavage of the pyrimidine component followed by a ring closure formation of 1,2,4-oxadiazole to