Danilo Giribone - [14C]CH2N2: a suitable precursor for the preparation of 14C labeled anthracyclines

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      Publication Details (including relevant citation   information):

      C.Felicini,   D.Giribone, A.Pignatti, E.Fontana.

      Journal of Labelled Compounds   and Radiopharmaceuticals, (2002) 45:   1184-1186

      Abstract:

      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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