Radiosyntheses of labeled beta-pseudothymidine ([C-11]- and [H-3]methyl) and its biodistribution and metabolism in normal and tumored mice.

@article{Grierson1995RadiosynthesesOL,
  title={Radiosyntheses of labeled beta-pseudothymidine ([C-11]- and [H-3]methyl) and its biodistribution and metabolism in normal and tumored mice.},
  author={J. Grierson and A. Shields and M. Zheng and S. Kozawa and J. Courter},
  journal={Nuclear medicine and biology},
  year={1995},
  volume={22 5},
  pages={
          671-8
        }
}
In order to develop labeled probes for measuring DNA synthetic rates in vivo we investigated [H-3]- and [C-11]methyl labeled beta-pseudothymidine (2a), and report on their radiosyntheses from methyl iodide. We find methylation is rapid and regioselective on N-1 of the acylurea moiety of 2'-deoxy-beta-D-pseudouridine (1a), in the presence of N,N-diisopropylethylamine and N,N-dimethylformamide at 60 degrees C. Although yields are low (11% [C-11]-decay corrected and 4.4% [H-3]), the method is… Expand
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