Method for the preparation of 9-amino camptothecin

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United States of America Patent

PATENT NO 5840899
SERIAL NO

08602792

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.

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Patent Owner(s)

  • PHARMACIA ITALIA S.P.A.;PHARMACIA S.P.A.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bedeschi, Angelo Milan, IT 41 163
Cabri, Walter Rozzano, IT 98 223
Candiani, Ilaria Busto Arsizio, IT 29 105
Zarini, Franco Settimo Milanese, IT 21 87

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