Camptothecin derivatives, preparations thereof and antitumor age

Details Camptothecin derivatives, preparations thereof and antitumor age Camptothecin derivatives, preparations thereof and antitumor age

1997-11-21

1998-12-01

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546 70, C07D48702

Patent

active

058439544

ABSTRACT:
New camptothecin derivatives of the general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen or a C.sub.1 -C.sub.6 alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, C.sub.2 -C.sub.6 acyloxy or methoxyethoxymethoxy group, R.sup.4 represents a hydrogen or halogen atom, and R.sup.5 represents a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 unsaturated alkyl, alkylthioalkyl, alkoxyalkyl, pyridyl or substituted phenyl group, with the proviso that all of the R.sup.2, R.sup.3 and R.sup.4 substituents should not be a hydrogen atom, and a process for preparing the new camptothecin derivatives by subjecting the camptothecin derivatives of the general formula (2): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the same meanings as given above, to the reaction with N,N-dimethylethylenediamine without solvent to open the E-lactone ring followed by acylation of 17-hydroxyl group with corresponding acylating agents and an antitumor agent containing the same as an active ingredient.

REFERENCES:
patent: 4914205 (1990-04-01), Sawada et al.
patent: 5122606 (1992-06-01), Wani et al.
Yaegashi, et al Chem Pharm Bull vol. 42, No. 12 pp. 2518-2825 (Dec. 1994).
Seigo Sawada et al., "Chemical Modification of an Antitumor Alkloid, 20(S)-Camptothecin: E-Lactone Ring-Modified Water-Soluble Derivatives of 7-Ethylcamptothecin", Chem. Pharm. Bull. 41(2):310-313, 1993.

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