1421518-25-3

Basic information

• Product Name: N-(2-((4,6-dimorpholino-1,3,5-triazin-2-yl)amino)-4-methoxyphenyl)-2,2-difluoroacetamide
• Synonyms: N-(2-((4,6-dimorpholino-1,3,5-triazin-2-yl)amino)-4-methoxyphenyl)-2,2-difluoroacetamide
• CAS NO: 1421518-25-3
• Molecular Weight: 465.46
• Mol File: 1421518-25-3.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: N-(2-((4,6-dimorpholino-1,3,5-triazin-2-yl)amino)-4-methoxyphenyl)-2,2-difluoroacetamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(2-((4,6-dimorpholino-1,3,5-triazin-2-yl)amino)-4-methoxyphenyl)-2,2-difluoroacetamide(1421518-25-3)
• EPA Substance Registry System: N-(2-((4,6-dimorpholino-1,3,5-triazin-2-yl)amino)-4-methoxyphenyl)-2,2-difluoroacetamide(1421518-25-3)

Safety Data

• Hazardous Substances Data: 1421518-25-3(Hazardous Substances Data)

Upstream product

• 7597-22-0 2-chloro-4,6-di-morpholin-4-yl-[1,3,5]triazine 
• 381-72-6 difluoroacetyl chloride 
• 1421518-23-1 N₁-(4,6-dimorpholino-1,3,5-triazin-2-yl)-5-methoxybenzene-1,2-diamine 
• 1421518-21-9 N-(5-methoxy-2-nitrophenyl)-4,6-dimorpholino-1,3,5-triazin-2-amine 

Relevant articles and documents

Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase

Phosphoinositide 3-kinases (PI3K) hold significant therapeutic potential as novel targets for the treatment of cancer. ZSTK474 (4a) is a potent, pan-PI3K inhibitor currently under clinical evaluation for the treatment of cancer. Structural studies have shown that derivatisation at the 5- or 6-position of the benzimidazole ring may influence potency and isoform selectivity. However, synthesis of these derivatives by the traditional route results in a mixture of the two regioisomers. We have developed a straightforward regioselective synthesis that gave convenient access to 5- and 6-methoxysubstituted benzimidazole derivatives of ZSTK474. While 5-methoxy substitution abolished activity at all isoforms, the 6-methoxy substitution is consistently 10-fold more potent. This synthesis will allow convenient access to further 6-position derivatives, thus allowing the full scope of the structure-activity relationships of ZSTK474 to be probed.