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Synthesis of a 35 S‐labeled dinucleoside phosphorothioate prodrug, an orally bioavailable anti‐HBV agent
Author(s) -
Rhee SungWhi,
Iyer Radhakrishnan P.,
Coughlin John E.,
Padmanabhan Seetharamaiyer,
Malerich Jeremiah P.,
Tanga Mary J.
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2925
Subject(s) - chemistry , prodrug , bioavailability , reagent , radiochemistry , combinatorial chemistry , nuclear chemistry , pharmacology , organic chemistry , biochemistry , medicine
The 35 S‐labeled, dinucleoside phosphorothioate 1, an orally available agent against hepatitis B virus, was prepared in eight steps with high specific activity and radiochemical purity. Radiolabeled 3 H ‐benzodithiole‐3‐one‐1,1‐dioxide was synthesized in four steps from 35 S 8 and was used as the sulfurizing reagent. Copyright © 2012 John Wiley & Sons, Ltd.