1022964-40-4

Upstream product

• 3932-97-6 2,4-dichloro-5-trifluoromethylpyrimidine 
• 4141-08-6 2-Amino-N-methylbenzamid 

Downstream Products

• 1257993-27-3 2-{[2-({4-[(dimethylphosphoryl)methyl]phenyl}amino)-5-(trifluoromethyl)pyrimidin-4-yl]amino}-N-methylbenzamide 
• 1257994-47-0 diethyl (2-fluoro-5-methoxy-4-{[4-{[2-(methylcarbamoyl)phenyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}benzyl)phosphonate 
• 1257994-79-8 diethyl [methoxy(4-{[4-{[2-(methylcarbamoyl)phenyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)methyl]phosphonate 
• 1257994-78-7 diethyl [ethoxy(4-{[4-{[2-(methylcarbamoyl)phenyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)methyl]phosphonate 
• 1257993-35-3 diethyl (4-{[4-{[2-(methylcarbamoyl)phenyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}benzyl)phosphonate 

Relevant academic research and scientific papers

Synthesis and biological evaluation of new pyrimidine derivatives as fak inhibitors for development of antitumor agents

In this paper, a set of new pyrimidine derivatives was designed and synthesized. Subsequently, all the final targets were evaluated for antitumor activities in vitro on four human cancer cell lines including U-87 MG, MDA-MB-231, PC-3, and MCF-7, which were high expressed with focal adhesion kinase (FAK). The results were shown that these compounds performed well antitumor activities. Especially 2-((2-((4-((2-((2-acrylamidoethyl)amino)-3,4-dioxocyclobut-1-en-1-yl)amino)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylbenzamide (7b) exhibited the highest antitumor activities with 2.16 μM, 2.03 μM, 6.19 μM, and 21.31 μM, respectively. In addition, all the compounds were tested activities against FAK and compound 7b was also the best candidate with IC50 value of 5.9 nM.

5-trifluoromethylpyrimidine derivative and preparation method and application thereof

The invention relates to a 5-trifluoromethylpyrimidine derivative and a preparation method and application thereof. The structural formula R of the 5-trifluoromethylpyrimidine derivative is selected from the 5-trifluoromethylpyrimidine derivative disclosed by the invention, is novel in structure, has relatively good water solubility, has a relatively strong inhibition effect on tumor cells, and has a very good application prospect in preparation of anti-tumor drugs.

FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND C-MET INHIBITORS

The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.