25713-57-9

Upstream product

• 108-77-0 1,3,5-trichloro-2,4,6-triazine 
• 100-53-8 phenylmethanethiol 

Downstream Products

• 1391926-35-4 4-(4-(benzylsulfonyl)-6-(2-(tetrahydro-2H-pyran-2-yl)-2H-indazol-4-yl)-1,3,5-triazin-2-yl)morpholine 
• 1391926-34-3 4-(4-(benzylthio)-6-(2-(tetrahydro-2H-pyran-2-yl)-2H-indazol-4-yl)-1,3,5-triazin-2-yl)morpholine 
• 1391926-33-2 4-(4-(benzylthio)-6-chloro-1,3,5-triazin-2-yl)morpholine 
• 1042726-66-8 2-benzylthio-4-amino-6-ethynyl-1,3,5-triazine 
• 1092455-72-5 C₁₅H₁₈N₄SSi 
• 30360-85-1 6-benzylsulfanyl-[1,3,5]triazine-2,4-diamine 
• 1042726-64-6 2-benzylsulfanyl-4-chloro-6-(trimethylsilyl)ethynyl-1,3,5-triazine 

Relevant academic research and scientific papers

Discovery of Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines

A new class of potent PI3Kα inhibitors is identified based on aryl substituted morpholino-triazine scaffold. The identified compounds showed not only a high level of enzymatic and cellular potency in nanomolar range but also high oral bioavailability. The three lead molecules (based on their in vitro potency) when evaluated further for in vitro metabolic stability as well as pharmacokinetic profile led to the identification of 26, as a candidate for further development. The IC50 and EC50 value of 26 is 60 and 500 nM, respectively, for PI3Kα enzyme inhibitory activity and ovarian cancer (A2780) cell line. The identified lead also showed a high level of microsomal stability and minimal inhibition activity for CYP3A4, CYP2C19, and CYP2D6 at 10 μM concentrations. The lead compound 26, demonstrated excellent oral bioavailability with an AUC of 5.2 μM at a dose of 3 mpk in mice and found to be well tolerated in mice when dosed at 30 mpk BID for 5 days.

Solid phase synthesis of novel biaryl triazine library by suzuki cross coupling

Two methods are used to produce diaryl trisubstituted triazines. In the first method, cyanuric chloride is first reacted with a 4-alkoxybenzylamine. The product of this reaction is then reacted with a resin-bound amine, such as 4-alkoxybenzylamine, to ens

Novel orthogonal strategy toward solid-phase synthesis of 1,3,5-substituted triazines.

[reaction: see text] To improve upon the previous orthogonal method for synthesis of a triazine library, an alternative strategy has been developed via oxidation-activation of the thioether to the sulfone. Through a comparison between these two methods, the sulfone strategy was demonstrated as an enhanced method in the generation of highly pure triazine library compounds.

Palladium-catalyzed cross-coupling reaction of resin-bound chlorotriazines

To introduce the biaryl structure as a triazine functionality, we have developed a new synthetic route via the Suzuki cross-coupling reaction of resin-bound chlorotriazines. The Suzuki cross-coupling reaction was achieved using various arylboronic acids, Pd(PPh3)4, Cs2CO3, and dioxane. With the integration of this chemistry and our previous orthogonal methodology, the triazine library is greatly expanded to a biaryl scaffold.