Process for preparing 3'-deamino analogs of glycoside...

C - Chemistry – Metallurgy – 07 – H

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260/208.2

C07H 15/24 (2006.01) C07H 15/252 (2006.01)

Patent

CA 1184903

ABSTRACT OF THE DISCLOSURE Antitumor anthracycline glycosides of the formula: Image wherein R1 is hydrogen or hydroxyl and R2 is the .alpha.-L-pyranosyl- hexose II or III Image II III are prepared from 3',4'-diepi-analogs of daunorubicin and doxo- rubicin by deamination in a cold acidic medium, such as 1N aqueous acetic and at 0°C with NaNO2. In this series of new anthracyclines showing antileukemic activity against murine leukemias, the doxo- rubicin analogs, when parenterally administered display an activity comparable or superior to that of doxorubicin and they are also active orally against Gross murine leukemia.

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