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

JA Hill, DD Bankston

Index: Hill; Bankston Journal of Labelled Compounds and Radiopharmaceuticals, 1995 , vol. 36, # 8 p. 713 - 718

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Abstract

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 ...