Tumor inhibiting [ 1 , Zbis ( fluorophenylethylenediamine ] platinum - ( II ) complexes . Part I : synthesis

  • Margaretha JENNERWEINi, Herta REILEi, Reiner LASKEi, Walter KRISCHKEi, Gunther BERNHARDTi, Thilo Spruss
  • Published 2004

Abstract

The synthesis of the diastereomeric 1,2-bis(2-,3and 4-fluorophenyl)ethylenediamines 4-6, lo-12 from meso-1,2-bis(2-hydroxyphenyl)ethylenediamine and 2-, 3and 4-fluorobenzaldehyde by a diaza-Cope-rearrangement and their conversion into the [1,2-bis(2-, 3and 4-fluorophenyl)ethylenediamine]dihaloplatinum (II) complexes (Hal = Cl, 13-M; Hal = I, 19-24) with K,PtHal, is described. From the diiodoplatinum(I1) complexes (19-24) the better water soluble diaqua[l,Zbis(2-, 3and 4-fluorophenyl)ethylenediamine]platinum(II) sulfates (25-30) and [1,2-bis(4fluorophenyl)ethylenediamine]dinitratoplatinum (II) complexes (31 and 32) are obtained by reacting with Ag2S04 or AgNOs. On the P388Di leukemia cell line the racemic platinum (II) complexes are more active than their meso-analogues and equiactive with cis-platin. The position of the fluorine atom and the kind of the leaving group do not influence the activity.

Cite this paper

@inproceedings{JENNERWEINi2004TumorI, title={Tumor inhibiting [ 1 , Zbis ( fluorophenylethylenediamine ] platinum - ( II ) complexes . Part I : synthesis}, author={Margaretha JENNERWEINi and Herta REILEi and Reiner LASKEi and Walter KRISCHKEi and Gunther BERNHARDTi and Thilo Spruss}, year={2004} }