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A general synthesis of 2′‐deoxy‐2′‐[ 18 F]fluoro‐1‐ β ‐D‐arabinofuranosyluracil and its 5‐substituted nucleosides
Author(s) -
Alauddin Mian M.,
Conti Peter S.,
Fissekis John D.
Publication year - 2003
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.637
Subject(s) - chemistry , radiochemistry , stereochemistry
Several 2′‐deoxy‐2′‐[ 18 F]fluoro‐1‐ β ‐D‐arabinofuranosyluracil derivatives have been synthesized. Coupling of 1‐bromo‐2‐deoxy‐2‐[ 18 F]fluoro‐3,5‐di‐O‐benzoyl‐ α ‐D‐arabinofuranose 2 with protected uracil derivatives 3a–e followed by hydrolysis and high‐performance liquid chromatography purification produced the radiolabeled nucleosides 4a–e in 15–30% yield (d. c.), >99% radiochemical purity and 55.5–103.6 GBq/µmol specific activities. Copyright © 2003 John Wiley & Sons, Ltd.