6533b7dcfe1ef96bd1272b8b

RESEARCH PRODUCT

The Di-Tert-Butyl Oxymethylphosphonate Route to the Antiviral Drug Tenofovir

B. Frank GuptonJule-phillip DietzTill OpatzTimothy F. JamisonDorota Ferenc

subject

Tert butylTenofovirmedicine.drug_classChemistryTwo stepCombinatorial chemistryPhosphonatechemistry.chemical_compoundReaction sequenceElectrophilemedicineAdefovirAntiviral drugmedicine.drug

description

<div>The present manuscript describes a simple, two step synthesis of tenofovir from HPA through phosphonomethalation with a novel doubly protected oxymethylphosphonate electrophile. The crystalline electrophile can be prepared in a simple reaction sequence and can be deblocked more easily than its ditehyl analogue involved in the current commercial process for making the drug.</div><div>The approach is general and can also be used for the preparation of related antivirals and the synthesis of adefovir is described as well.<br></div>

https://doi.org/10.26434/chemrxiv.12957935