213772-53-3

Upstream product

• 4048-33-3 6-amino-1-hexanol 
• 204773-56-8 Toluene-4-sulfonic acid 5-(benzyl-tert-butoxycarbonyl-amino)-pentyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 213772-26-0 benzyl-(5-oxo-pentyl)-carbamic acid tert-butyl acid 
• 100-52-7 benzaldehyde 
• 2937-99-7 N-benzyl-5-aminopentan-1-ol 
• 2508-29-4 5-hydroxypentylamine 
• 213771-60-9 tert-Butyl N-benzyl-5-hydroxypentylcarbamate 
• 208244-48-8 5-{[1-Phenyl-meth-(E)-ylidene]-amino}-pentan-1-ol 

Downstream Products

• 305351-57-9 N-(N'-benzyl-N'-tert-butoxycarbonyl-5-aminopentyl)-N-tert-butoxycarbonyl-6-aminopentanoyl-1-toluene-4-sulfonic acid 
• 213773-01-4 N-(N'-benzyl-N'-tert-butoxycarbonyl-5-aminopentyl)-N-tert-butoxycarbonyl-6-aminohexanoic acid 

Relevant academic research and scientific papers

Pyrimidinone-1,3-oxathiolane derivatives with antiviral activity

Compounds of formula (I) wherein Ra and Rb the same or different, are hydrogen atoms, acyl groups deriving from a lower carboxylic acid or chains of formula (a) useful as reverse transcriptase inhibitors antiviral activity are described.

Synthesis and anti-HIV evaluation of new 2',3'-dideoxy-3'-thiacytidine prodrugs

A series of anti-HIV prodrugs possessing various polyaminated side arms have been developed. The incorporation of a N-Boc protected monoamine or diamine side arm into the backbone of the 2',3'-dideoxy-3'-thiacytidine 1 (BCH-189) provided an increase in antiviral potency, which could be several orders magnitude greater than the parent drug (1) depending on the cell culture systems used (MT-4 or MDMs). Twenty six 2',3'-dideoxy-3'-thiacytidine prodrugs which differ from each other by the length, the nature of the 5'-O function and the 5'-O or/and N-4 position on the nucleoside moiety were synthesized. Among this new series of prodrugs, several congeners (12c and 12a) were found to inhibit HIV-1 replication in cell culture with 50% effective concentrations EC50 of 10 and 50 nM respectively, in MT-4 cells. Compound 12c was found more active on infected MDMs cells with 50% effective concentration of 0.01 nM. The synthesis and the antiviral properties of these compounds are discussed.