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Synthesis of tritium-labelled 5-chloro-2′,3′-dideoxy-3′-fluorouridine (935u83) - a selective anti-HIV agent

✍ Scribed by John A. Hill; Donald D. Bankston

Publisher: John Wiley and Sons
Year: 1995
Tongue: French
Weight: 279 KB
Volume: 36
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580360802

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✦ Synopsis

Abstract

[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%.

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