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- W2886757686 abstract "Abstract To 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 [D 8 ]9‐(2‐hydroxypropyl)adenine (racemic R/S‐HPA) using a 10%Pd/C & PtO 2 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 [D 8 ]9‐[2‐phosphonomethoxypropyl]adenine ([D 8 ] R/S‐PMPA) in two steps. Using [D 8 ] R/S‐PMPA as a common intermediate, thus, we further synthesized [D 8 ] R/S‐tenofovir disoproxil fumarate and [D 8 ]tenofovir alafenamide in 2–3 steps with 60% and 20% overall yield, respectively." @default.
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- W2886757686 date "2018-08-14" @default.
- W2886757686 modified "2023-09-27" @default.
- W2886757686 title "An Efficient Pd & Pt‐Catalyzed H/D Exchange Approach towards the Synthesis of Deuterium‐Labeled Antiviral Prodrugs, Tenofovir Disoproxil Fumarate and <b>Tenofovir Alafenamide</b>" @default.
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- W2886757686 doi "https://doi.org/10.1002/slct.201801990" @default.
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