Process for the preparation of 9-amino camptothecin

Details Process for the preparation of 9-amino camptothecin Process for the preparation of 9-amino camptothecin

1994-09-28

1997-03-25

Daus, Donald

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D491147

Patent

active

056146280

ABSTRACT:
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.

REFERENCES:
Journal of Medicinal Chemistry, vol. 34, No. 1, 1991, pp. 98-107, William D. Kingbury, et al., "Synthesis of Water-Soluble (Aminoalkyl)Camptothechin Analogues: Inhibition of Topoisomerase I and Antitumor Activity".
Journal of Medicinal Chemistry, 1986, vol. 29, No. 11, Mansukh C. Wani, et al., "Plant Antitumor Agents. 23. Synthesis and Antileukemic Activity of Camptothecin Analogues", pp. 2358-2363.

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