849778-77-4

Upstream product

• 24630-68-0 diisopropyl hydroxymethylphosphonate 
• 1809-20-7 diisopropyl hydrogenphosphonate 
• 934497-45-7 benzoic acid 4-(tert-butyl-dimethyl-silanyloxy)-2-hydroxy-tetrahydro-furan-3-yl ester 
• 934497-20-8 2′-O-benzoyl-3-O-tert-butyldimethylsilyl-L-threonolactone 
• 91345-19-6 2′-O-benzoyl-L-threonolactone 
• 134963-85-2 (diisopropoxyphosphoryl)methyl trifluoromethanesulfonate 
• 1446785-56-3 N⁶-benzoyl-9-(2′-O-benzoyl-α-L-threofuranosyl)adenine 
• 849779-01-7 1α,2-O-benzoyl-3-O-(diisopropylphosphonomethyl)-L-threose 
• 60855-35-8 6-benzoylamino-9-trimethylsilylpurine 

Downstream Products

• 1019983-66-4 1-(adenin-9-yl)-2-O-phenoxythiocarbonyl-3-O-(diisopropylphosphonomethyl)-L-threose 

Relevant academic research and scientific papers

NOVEL ANTIVIRAL COMPOUNDS, A PROCESS FOR THEIR PREPARATION, AND THEIR USE FOR TREATING VIRAL INFECTIONS

The present invention relates to novel pro-drugs of L-2'-deoxythreose nucleoside phosphonates, such as phosphoramidate, phosphorodiamidate and phospho-diester prodrugs. The invention also relates to a process for preparing these novel prodrugs of nucleoside phosphonates. The invention also relates to the use of these novel phosphonatemodified nucleosides to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses belonging to the HBV family.

Amidate Prodrugs of Deoxythreosyl Nucleoside Phosphonates as Dual Inhibitors of HIV and HBV Replication

The synthesis of four l-2′-deoxy-threose nucleoside phosphonates with the natural nucleobases adenine, thymine, cytosine, and guanosine has been performed. Especially the adenine containing analogue (PMDTA) was endowed with potent antiviral activity displ

Deoxythreosyl phosphonate nucleosides as selective anti-HIV agents

Out of a series of eight new phosphonate nucleosides with an L-threose and an L-2-deoxythreose sugar moiety, two new compounds were identified (PMDTA and PMDTT) that showed potent anti-HIV-1 (HIV-2) activity [EC50 = 2.53 μM (PMDTA) and 6.59 μM (PMDTT)], while no cytoxicity was observed at the highest concentration tested [CC50 > 316 μM (PMDTA) and > 343 μM (PMDTT)]. The kinetics of incorporation of PMDTA into DNA (using the diphosphate of PMDTA as substrate and HIV-1 reverse transcriptase as catalyst) was similar to the kinetics observed for dATP, while the diphosphate of PMDTA was a very poor substrate for DNA polymerase α. The incorporated PMDTA fits very well in the active site pocket of HIV-1 reverse transcriptase.

PHOSPONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION

The present invention relates to novel phosponate nucleosides, more specifically to novel phosponalkoxy substituted nucleosides. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to