Tumor Inhibiting [1,2‐Bis(difluorophenyl)ethylenediamine]‐dichloroplatinum(II) Complexes, I: Synthesis

The synthesis of the diastereomeric 1,2‐bis(2,3‐, 2,4‐, 2,5‐, 2,6‐, 3,4‐, 3,5‐difluorophenyl)ethylenediamines (meso, D/L 8—13 ) from meso 1,2‐bis(2‐hydroxyphenyl)ethylenediamine and the respective difluorobenzaldehyde by a diaza‐ Cope ‐rearrangement and their conversion into the [1,2‐bis(2,3‐, 2,4‐, 2,5‐, 2,6‐, 3,4‐, 3,5‐difluorophenyl)ethylenediamine]dihaloplatinum(II)‐complexes (meso D/L 8—13 PtCl 2 ; meso D/L 9 ‐ and 11 ‐PtI 2 ) with K 2 PtHal 4 (Hal = Cl, I) is described. From the diiodoplatinum(II)‐complexes (meso D/L 9 ‐and 11 ‐Ptl 2 ) the better water soluble diaqua[1,2‐bis(2,4‐ and 2,6‐difluorophenyl)ethylenediamine]platinum(II) sulfates (meso, D/L 9 ‐ and 11 ‐PtSO 4 ) are obtained by reaction with Ag 2 SO 4 .