Journal of fluorine chemistry

Synthesis of 3′-fluoro-3′-deoxythymidine and studies of its 18F-radiolabeling, as a tracer for the noninvasive monitoring of the biodistribution of drugs against AIDS

IK Wilson, S Chatterjee, W Wolf

Index: Wilson, I. K.; Chatterjee, S.; Wolf, W. Journal of Fluorine Chemistry, 1991 , vol. 55, # 3 p. 283 - 289

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Citation Number: 39

Abstract

Abstract 3′-Fluoro-3′-deoxy-thymidine (FDT), a fluorinated analog of 3′-azido-thymidine (AZT), is both more active against the HIV virus but also more toxic than AZT. Because of its fluorine atom, it can be labeled with 18 F to be used to monitor this drug's biodistribution and targeting. A new synthesis for FDT, suited for 18 F labeling, has been developed. After protecting the 5′-hydroxy group with a trityl group, the 3′-hydroxy group was subtituted ...