41552-92-5

Upstream product

• 80585-34-8 9-(2,3,5-tri-Ο-acetyl-1β-D-ribofuranosyl)-6-(piperidin-1-yl)-9H-purine 
• 110-89-4 piperidine 
• 2004-06-0 6-Chloropurine riboside 
• 1928-81-0 6-(piperidin-1-yl)-9H-purine 
• 13035-61-5 1,2,3,5-tetraacetylribose 
• 6091-44-7 piperidine hydrochloride 
• 385806-21-3 9-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-6-(imidazol-1-yl)purine 
• 3181-38-2 2',3',5'-tri-O-acetylinosine 
• 309253-78-9 6-(1H-imidazol-1-yl)-9-(β-D-ribofuranosyl)purine 

Relevant academic research and scientific papers

Discovery of 6-[4-(6-nitroxyhexanoyl)piperazin-1-yl)]-9H-purine, as pharmacological post-conditioning agent

Novel purine analogues bearing nitrate esters were designed and synthesized in an effort to develop compounds triggering endogenous cardioprotective mechanisms such as ischemic preconditioning (IPC) or postconditioning (PostC). The majority of the compounds reduced infarct size compared to the control group in anesthetized rabbits, whereas administration of the most active analogue 16 at a dose of 3.8 μmol/kg resulted on a significant reduction of infarct size, compared to PostC group (13.4 ± 1.9% vs 26.4 ± 2.3%). These findings introduce a novel class of promising pharmacological compounds that could be used as mimics or enhancers of PostC.

6-Substituted purines as ROCK inhibitors with anti-metastatic activity

Rho-associated serine/threonine kinases (ROCKs) are principal regulators of the actin cytoskeleton that regulate the contractility, shape, motility, and invasion of cells. We explored the relationships between structure and anti-ROCK2 activity in a group

HFIP Promoted Low-Temperature SNAr of Chloroheteroarenes Using Thiols and Amines

A highly efficient and an unprecedented hexafluoro-2-propanol, promoting low-temperature aromatic nucleophilic substitutions of chloroheteroarenes, has been performed using thiols and (secondary) amines under base-free and metal-free conditions. The developed protocol also provides excellent regio-control for the selective functionalization of dichloroheteroarenes, while the utility of the protocol was demonstrated by the modification of a commercially available drug ceritinib.

Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes

A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields.

Testing nucleoside analogues as inhibitors of Bacillus anthracis spore germination in vitro and in macrophage cell culture

Bacillus anthracis, the etiological agent of anthrax, has a dormant stage in its life cycle known as the endospore. When conditions become favorable, spores germinate and transform into vegetative bacteria. In inhalational anthrax, the most fatal manifest

Anti-HCV nucleoside derivatives

The present invention comprises novel and known purine and pyrimidine nucleoside derivatives which have been discovered to be active against hepatitis C virus (HCV). The use of these derivatives for the treatment of HCV infection is claimed as are the novel nucleoside derivatives disclosed herein.

Mild and efficient functionalization at C6 of purine 2′-deoxynucleosides and ribonucleosides

(Equation Presented) Treatment of sugar-protected inosine and 2′-deoxyinosine derivatives with a cyclic secondary amine or imidazole and I2/Ph3P/EtN(i-Pr)2/(CH2-Cl 2 or toluene) gave quantitative conversions into 6-N-(substituted)purine nucleosides. SNAr reactions with (imidazol-1-yl) derivatives gave 6-(N, O, or S)-substituted products. The 6-(benzylsulfonyl) group underwent SNAr displacement with an arylamine at ambient temperature.