Process for the preparation of 9-amino camptothecin

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United States of America Patent

PATENT NO 5614628
SERIAL NO

08313906

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Abstract

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A process for preparing 9-amino camptothecin comprising the steps of: (1) reacting a compound of formula (III) ##STR1## wherein the hydroxy group on ring A is in the 10- or 12-position, with a nitrating agent, to form the corresponding 9-nitro compound; (2) converting the 9-nitro compound into a corresponding compound of formula (V) ##STR2## wherein XO is a group that can be removed reductively; and (3) reductively removing the XO group and reducing the nitro group of the compound of formula (V), to form the 9-amino camptothecin, a known antitumor compound. The present invention also includes compound having the above formula (V) and their 9-amino analogs, which have antitumor activity.

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Patent Owner(s)

Patent OwnerAddress
PHARMACIA ITALIA S P AVIA ROBERT KOCH 1 2 20152 MILAN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bedeschi, Angelo Milan, IT 41 168
Cabri, Walter Rozzano, IT 98 224
Candiani, Ilaria Arsizio, IT 30 107
Penco, Sergio Milan, IT 68 415
Zarini, Franco Milanese, IT 21 87

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