Publication Details (including relevant citation information):
C.Felicini, D.Giribone, A.Pignatti, E.Fontana.
Journal of Labelled Compounds and Radiopharmaceuticals, (2002) 45: 1184-1186
Since the discovery of the antitumoral activity of daunorubicin and doxorubicin in clinical trials, anthracyclines have been intensively investigated to find new analogs with a broader spectrum of activity and/or reduced toxicity. in order to perform the distribution, pharmacokinetics, and metabolism studies of these compounds, the preparation of 14C-labelled materials was required. To date several anthracyclines were successfully synthesized in our company using [14C]diazomethane as radiolabelled precursor, and the stability of the C14 position was found to be quite satisfactory in-vivo. In this paper an overview of the strategy used in our labs to successfully introduce 14C in the anthracyclines structures is described.
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