Daunorubicin and doxorubicin labelled with .sup.14 C at the 14-p

Details Daunorubicin and doxorubicin labelled with .sup.14 C at the 14-p Daunorubicin and doxorubicin labelled with .sup.14 C at the 14-p

1978-02-14

1980-07-08

Brown, Johnnie R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

424180, 536 4, C07H 1524

Patent

active

042118646

ABSTRACT:
[14-.sup.14 C]-daunorubicin and doxorubicin are prepared by reacting 9-desacetyl-9-formyl-N-trifluoroacetyl daunorubicin with [.sup.14 C]-diazomethane to form [14-.sup.14 C]-N-trifluoroacetyl daunorubicin from which the protecting group is removed by mild alkaline hydrolysis to afford [14-.sup.14 C]-daunorubicin which is then, in the form of the hydrochloride, reacted with bromine to form the corresponding labelled 14-bromo derivative, which, upon treatment with sodium formate leads to [14-.sup.14 C]-doxorubicin.

REFERENCES:
patent: 3803124 (1974-04-01), Arcamone et al.
patent: 3945993 (1976-03-01), Schaffner et al.

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