MIXED CIS-DIAMINODICHLORODIHYDROXO PLATINUM (IV) COMPLEXES HAVING ANTITUMOR ACTIVITY Russian patent published in 1996 - IPC

FIELD: medicine. SUBSTANCE: complex platinum compounds, more particularly cis-diaminodichlorodihydroxo platinum (4+) complexes contain as substituent CH₃, C₂H₅, iso--C₃H₇ or tert- butylamine and have antitumor activity. Synthesis is carried out by oxidizing alkylaminochloroaminochloro platinum (2+) complex with H₂O₂ in water, while heating for 10 min and subsequently adding MnO₂ and maintaining the mixture at room temperature for 2.5 h till oxygen bubbles cease to liberate. On heating and separating MnO₂, the filtrate is maintained over P₂O₅ till volume is reduced by 4 times and desired complex crystals are separated. Yield, %; color; decomp. temperature, C; solubility, mmole/l; electrical conduction after 10 min and 48 h, sq.cm*ohm, mole: (a) 57, pale yellow, 160; 26.2; 0.7; 2.3; (b) 61; yellow, 185; 32.5; 2.4; 2.5; (c) 74, pale yellow, 175, 20.9; 1.3; 3.1; (d) 83, bright yellow, 198; 14; 0.8; 3.1. These agents inhibit development of sarcoma tumors and other diseases by 86.9- 96.3% at dose of 20-25 mg/kg as against 83% for oxoplatinum. Toxicity LD₅₀, mg/kg: (a) 123; (b) 128; (c) 52; (d) 22. EFFECT: improved properties . 8 tbl