Platinum(II) complex and processes for preparing the same

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

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549450, 549451, 556137, C07F 1500, C07D31700

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active

053959477

ABSTRACT:
Disclosed herein are novel platinum(II) complexes having a potent anti-tumor activity which are represented by the formula (1), ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are a hydrogen atom or a C.sub.1-4 alkyl group, respectively, or jointly form a cycloalkane group together with the carbon atom attached thereto; two Xs jointly form a group represented by formula (a) or (b) wherein, R.sub.3 is a hydrogen atom or a methyl group; R.sub.4 and R.sub.5, which may be the same or different, are a hydrogen atom or a C.sub.1-4 alkyl group, respectively, or jointly form a cyclobutane together with the carbon thereto; and the absolute configurations at the respective chiral centers in the 4,5-bis(aminomethyl)-1,3-dioxolane moiety are (4R,5R) or (4S,5S); processes for the preparing the same; and their use for treating animal or human cancer. Further, disclosed herein are novel intermediates useful for the preparation of the platinum(II) complexes and processes for preparing said intermediates.

REFERENCES:
patent: 4665210 (1987-05-01), Bitha et al.
patent: 4730069 (1988-03-01), Kolar et al.
patent: 4783452 (1988-11-01), Haines et al.
patent: 4870070 (1989-09-01), Bitha et al.
Rosenberg et al., Nature 222, 385, 1969.
Peter W. Feit et al., J. Med. Chem. 7, 14, 1964.
Cancer Chemotheraphy Reports, Part 3, 3(2), 7, 1972.

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