76746-74-2

Upstream product

• 420-04-2 CYANAMID 
• 104-94-9 4-methoxy-aniline 

Downstream Products

• 677752-89-5 4-{4-[2-(4-methoxy-phenylamino)-pyrimidin-4-yl]-benzenesulfonyl}-piperazine-1-carboxylic acid tert-butyl ester 
• 1383074-12-1 N-(4-methoxyphenyl)-4-(1-methyl-1H-benzimidazol-2-yl)pyrimidin-2-amine 
• 1215292-25-3 2-(4-methoxyanilino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-one 
• 1215292-50-4 2-(4-methoxyanilino)-5,7-dihydro-6H-pyrido[3,2-b]pyrimido[4,5-d]azepin-6-one 
• 1215292-45-7 2-(4-methoxyanilino)-5,7-dihydro-6H-pyrido[4,3-b]pyrimido[4,5-d]azepin-6-one 
• 1215292-39-9 2-(4-methoxyanilino)-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-one 

Relevant academic research and scientific papers

7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones designed by a “cut and glue” strategy are dual aurora a/vegf-r kinase inhibitors

Although overexpression and hyperactivity of protein kinases are causative for a wide range of human cancers, protein kinase inhibitors currently approved as cancer drugs address only a limited number of these enzymes. To identify new chemotypes addressing alternative protein kinases, the basic structure of a known PLK1/VEGF-R2 inhibitor class was formally dissected and reassembled. The resulting 7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones were synthesized and proved to be dual inhibitors of Aurora A kinase and VEGF receptor kinases. Crystal structures of two representatives of the new chemotype in complex with Aurora A showed the ligand orientation in the ATP binding pocket and provided the basis for rational structural modifications. Congeners with attached sulfamide substituents retained Aurora A inhibitory activity. In vitro screening of two members of the new kinase inhibitor family against the cancer cell line panel of the National Cancer Institute (NCI) showed antiproliferative activity in the single-digit micromolar concentration range in the majority of the cell lines.

C-H activation at a bidentate ligand coordinated to palladium(II) - An electrophilic attack supported by an external base

2-(2-Phenylaminopyrimidin-4-yl)pyridines undergo C-H activation at the phenyl ring in the ortho position to the amine nitrogen atom when reacted with (PhCN)2PdCl2 and finally form N,N,C-coordinated palladium(II) complexes in high yields. Five differently substituted complexes were synthesized and characterized by spectroscopy and X-ray structure analysis. The reaction mechanism for the formation of these complexes was elucidated by kinetic experiments, which allowed the calculation of the activation parameters of the complex formation.

C-H activation at a bidentate ligand coordinated to palladium(II) - An electrophilic attack supported by an external base

2-(2-Phenylaminopyrimidin-4-yl)pyridines undergo C-H activation at the phenyl ring in the ortho position to the amine nitrogen atom when reacted with (PhCN)2PdCl2 and finally form N,N,C-coordinated palladium(II) complexes in high yields. Five differently substituted complexes were synthesized and characterized by spectroscopy and X-ray structure analysis. The reaction mechanism for the formation of these complexes was elucidated by kinetic experiments, which allowed the calculation of the activation parameters of the complex formation.

Pyrazolopyridine antiherpetics: SAR of C2′ and C7 amine substituents

A novel series of potent pyrazolo[1,5-a]pyridine inhibitors of herpes simplex virus 1 replication have been identified. Several complimentary synthetic methods were developed to allow facile access to a diverse set of analogs from common late stage interm

A novel series of potent and selective IKK2 inhibitors

A novel series of aminopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling.