Methods of preparing and purifying 9-nitro-20-camptothecin

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D491147

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059228776

ABSTRACT:
A method is disclosed for the preparation of 9-nitrocamptothecin which involves reacting 20-camptothecin with at least one inorganic nitrate salt and at least one acid effective in catalyzing the formation of a nitronium ion, where the reaction occurs at a temperature and for a time sufficient to form the 9-nitrocamptothecin. Also, methods of further purifying the 9-nitrocamptothecin by column chromatography or by reprecipatation is also disclosed.

REFERENCES:
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patent: 5731316 (1998-03-01), Cao
Cotton et al. "Advanced Inorganic Chemistry" Interscience, New York, 1962 pp. 264-265.
Sawada et al. Chem. Pharm Bull. vol 39 (No. 2) pp. 3183-3188 (1991).
J.V. Crivello, "Nitrations and Oxidations with Inorganic Nitrate Salts in Trifluoroacetic Anhydride" J. Org. Chem., vol. 46, No. 15, 1981.

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