J. S. Valsborg, L. Knutsen, I. Lundt*
May 1, 1995
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0
Influential Citations
4
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
The synthesis of [8- 14 C]-2,6-dichloro-9H-purine (2), a radiolabelled precursor for preparing 14 C-labelled nucleosides, is described. Triethyl [ 14 C]orthoformate was reacted with 4,5-diamino-2,6-dichloropyrimidine (1) in acetonitrile at 90 o C with methanesulfonic acid as catalyst to generate 2 in 84% radiochemical yield. Reaction of 2 with 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribofuranose produced [8- 14 C]-9-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)-2,6-dichloropurine (3) in 86% yield. The radiochemical purity of 3 was higher than 98% with a specific activity of 36 mCi/mmol. This method has general application to 14 C-labelling of purines in drug development