849779-01-7

Upstream product

• 98-88-4 benzoyl chloride 
• 849778-99-0 1α,2-di-o-tertbutyldimethylsilyl-3-O-(diisopropylphosphonomethyl)-L-threose 
• 134963-85-2 (diisopropoxyphosphoryl)methyl trifluoromethanesulfonate 

Downstream Products

• 849778-79-6 1-(uracil-1-yl)-2-O-benzoyl-3-O-(diisopropylphosphonomethyl)-L-threose 
• 849778-78-5 1'α-(thymin-1-yl)-2'-O-benzoyl-3'-O-diisopropylphosphonomethyl-L-threose 
• 849778-80-9 1-(N⁴-acetylcytosin-1-yl)-2-O-benzoyl-3-O-(diisopropylphosphonomethyl)-L-threose 
• 849778-77-4 1'α-(N⁶-benzoyladenin-9-yl)-2'-O-benzoyl-3'-O-diisopropyl-phosphonomethyl-L-threose 

Relevant academic research and scientific papers

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