There are disclosed antitumor active 1,2-diphenyl-ethylenediamine)-platinum(II)-complex of the general formula ##STR1## wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl and R.sub.2 is either (1) a halogen atom and the groups R.sub.1, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydrogen C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, or R.sub.2 is (2) a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group in the 4-position or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and if R.sub.2 is (2) then the groups R.sub.1 and R.sub.3 which are the same or differnt are in the 2 and 6 positions of the phenyl group and are halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, a C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alklanoyloxy group or a halo or C.sub.1 -C.sub.5 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, with the proviso that R.sub.1 can also be hydrogen and the groups R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy group or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and X is the equivalent of a physiologically compatible anion and process of their production.

There are described (1-benzylethylenediamine)-platin(II)-complexes of the general formula: ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a benzyl group, or a phenylethyl group, and B is a thienyl radical, an indolyl radical, an imidazolyl radical, or a phenyl radical substituted by the radicals R.sub.5, R.sub.6, an R.sub.7 which are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, phenoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, C.sub.1 -C.sub.6 -alkanesulfonyloxy, carboxy, C.sub.1 -C.sub.6 -carbalkoxy, cyano, aminocarboxyl, aminocarbonyl, which contains one or two C.sub.1 -C.sub.6 -alkyl radicals, C.sub.1 -C.sub.6 -alkylcarbonyl, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, (C.sub.1 -C.sub.6 -alkyl).sub.3 N.sup.+, C.sub.1 -C.sub.6 -alkanoylamino, C.sub.1 -C.sub.6 -alkyl-C.sub.1 -C.sub.6 -alkanoylamino, C.sub.1 -C.sub.6 -alkanesulfonylamino, C.sub.1 -C.sub.6 -alkyl-C.sub.1 -C.sub.6 -alkanesulfonylamino, aminosulfonyl, aminosulfonyl which contains one or two C.sub.1 -C.sub.6 -alkyl radicals, C.sub.1 -C.sub.6 -alkoxysulfonyl (--SO.sub.2 --O--C.sub.1 --C.sub.6 -alkyl), sulfo (--SO.sub.3 H) or C.sub.1 -C.sub.6 -alkanesulfonyl and two of these groups can be the methylenedioxy group and X is the equivalent of a physiologically compatible anion, as well as optionally their salts with physiologically compatible cations and anions and process of their production.

The present invention comprises a water-soluble square-planar cis-platinum(II) four-coordinate complex having the formula: or wherein X is a monovalvent cation, two of which are present, selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethyglycinato; wherein Y is a divalent cation selected from the group consisting of citraconato, 1,1-cyclobutanedicarboxylato, 1,1-cyclopropanedicarboxylato, isocitratolactone and Z-iminodiacetato where Z is bound to the nitrogen and is ethyl, propyl, Isopropyl, n-butyl, sec-butyl, ter-butyl, n-amyl, isoamyl or OH. In one preferred aspect the water-soluble square-planar cis-platinum(II) four-coordinate complex has the formula: wherein X is a monovalent cation. Two X substituents are present in the platinum complex. These X substituents are preferably selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethylglycinato. Both X substituents are usually identical butmay be different.

The invention relates to a process for the treatment of tumors in animals with water soluble square-planar cis platinum(II) four-coordinate complexes comprising different nonovalent and divalent organic cations. Monovalent cations include galacturonato and N,N-dimethylglycinato and divalent cations include citraconato, 1,1-cyclobutanedicarboxylato, 1,1-cyclopropanedicarboxylato and Z-iminodiacetato where Z is bound to the nitrogen and is ethyl, propyl, isopropyl, n-butyl, secbutyl, ter-butyl, n-amyl, isoamyl or --OH. The treatment of animals comprises administering to the animals a pharmaceutical composition comprising a platinum complex of the composition described.

There is provided a method of synthesis of a radiolabelled platinum chemotherapeutic agent comprising the steps of: converting a metal halide to a radiolabelled platinum halide wherein the radiolabel is a radioisotope of Pt; and synthesizing the radiolabelled platinum chemotherapeutic agent from the radiolabelled platinum halide.