Abstract
AbstractTo support clinical bioequivalence (BE) studies of tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide fumarate (TAF), both deuterium‐labeled TDF and TAF (or their free bases, TD & TA) are highly desired for use as an internal standard. We have developed a method to prepare racemic [D8]9‐(2‐hydroxypropyl)adenine (racemic R/S‐HPA) using a 10%Pd/C & PtO2 catalyzed H−D exchange reaction as the key step to introduce the label in a highly efficient and cost‐effective way. The labeled R/S‐HPA was converted to racemic [D8]9‐[2‐phosphonomethoxypropyl]adenine ([D8] R/S‐PMPA) in two steps. Using [D8] R/S‐PMPA as a common intermediate, thus, we further synthesized [D8] R/S‐tenofovir disoproxil fumarate and [D8]tenofovir alafenamide in 2–3 steps with 60% and 20% overall yield, respectively.
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