Synthesis of PNU-159548 labelled with 14C and 2H

The cytotoxic antitumor compound PNU‐159548 (1) has been labelled with 14C and 2H. A three‐step sequence starting from [14‐14C]idarubicin (2a) led to radiochemically pure (>98%) [14‐14C]PNU‐159548 with a specific activity of 1.13 GBq/mmol. The synthesis of [2H4]PNU‐159548 was carried out in a sim...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2002-06, Vol.45 (7), p.543-550
Main Authors: Felicini, C., Fontana, E.
Format: Article
Language:English
Subjects:
alkycyclines
anthracyclines
antitumor agent
Biological and medical sciences
carbon-14
Contrast media. Radiopharmaceuticals
deuterium
Medical sciences
Pharmacology. Drug treatments
PNU-159548
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Summary:The cytotoxic antitumor compound PNU‐159548 (1) has been labelled with 14C and 2H. A three‐step sequence starting from [14‐14C]idarubicin (2a) led to radiochemically pure (>98%) [14‐14C]PNU‐159548 with a specific activity of 1.13 GBq/mmol. The synthesis of [2H4]PNU‐159548 was carried out in a similar manner starting from [1,1,2,2‐2H4]2‐bromoethanol (3b). Copyright © 2002 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.580