51944-25-3

Upstream product

• 5424-21-5 2,4-dichloro-6-methylpyrimidine 
• 62-53-3 aniline 
• 626-48-2 2,4-dihydroxy-6-methylpyrimidine 

Downstream Products

• 1207424-63-2 C₁₇H₂₃N₅ 
• 1207425-13-5 C₁₇H₁₇N₅ 
• 1207424-65-4 C₂₁H₂₉N₅O₂ 
• 1207981-86-9 C₂₁H₂₂N₆O₄S 

Relevant academic research and scientific papers

Regioselective 2-Amination of Polychloropyrimidines

The regioselective amination of substituted di- and trichloropyrimidines affording the 2-substituted products is reported. While aryl- and heteroarylamines require the use of a dialkylbiarylphosphine-derived palladium catalyst for high efficiency, more nucleophilic dialkylamines produce 2-aminopyrimidines under noncatalyzed SNAr conditions. The key is the use of 5-trimethylsilyl-2,4-dichloropyrimidine as a surrogate for the parent dichloropyrimidine. For more challenging cases, the 2-chloro-4-thiomethoxy analogues were prepared and exclusively afford the desired 2-aminated-4-thiomethoxypyrimidine products.

Synthesis, antimalarial activity, heme binding and docking studies of 4-aminoquinoline-pyrimidine based molecular hybrids

A series of novel 4-aminoquinoline-pyrimidine hybrids was synthesized and evaluated for their antimalarial activity. Several compounds showed potent antimalarial activity against both CQ-sensitive and CQ-resistant strains of P. falciparum with no cytotoxi

Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines

Two sets of diaminopyrimidines, totalling 45 compounds, were synthesized and assayed against Plasmodium falciparum. The SAR was relatively shallow, with only the presence of a 2-(pyrrolidin-1-yl)ethyl group at R2 significantly affecting activity. A subsequent series addressed high Log D values by introducing more polar side groups, with the most active compounds possessing diazepine and N-benzyl-4-aminopiperidyl groups at R1/R2. A final series attempted to address high in vitro microsomal clearance by replacing the C6-Me group with CF3, however antiplasmodial activity decreased without any improvement in clearance. The C6-CF3 group decreased hERG inhibition, probably as a result of decreased amine basicity at C2/C4.

Anilinopyrimidines as novel antituberculosis agents

A selection of novel anilinopyrimidine analogues have been found to have micromolar activity against Mycobacterium tuberculosis. This could potentially generate new lead compounds in the fight against multi-drug resistant tuberculosis.