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Synthesis of tritium‐labelled 5‐chloro‐2′,3′‐dideoxy‐3′‐fluorouridine (935u83) ‐ a selective anti‐HIV agent
Author(s) -
Hill John A.,
Bankston Donald D.
Publication year - 1995
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.2580360802
Subject(s) - chemistry , aldehyde , imidazolidine , tritium , adduct , reducing agent , radiochemistry , organic chemistry , catalysis , physics , nuclear physics
[5′‐ 3 H]‐5‐Chloro‐2′,3′‐diodeoxy‐3′‐fluorouridine ( 1 ; R = [ 3 H]) was prepared at a specific activity of 10.2 Ci/mmol suitable for development of a radioimmunoassay procedure. The synthetic sequence employed controlled oxidation of unlabelled 1 to the 5′‐aldehyde ( 2 ), isolation as the imidazolidine adduct ( 3 ), regeneration of the free aldehyde, reduction with [ 3 H]NaBH 4 , and purification by preparative TLC. The radiochemical purity was 98.0%.