Process for the preparation of trans- or cis-diammoniumdichlorodihydroxyplatinum(IV) salts and derivatives and their use for the preparation of pharmaceutical active agents

摘要

Production of trans- or cis-diammonium dichloro-dihydroxo-platinum (IV) (i.e. trans- or cis-oxoplatin) (A) or their derivatives involves reacting trans- or cis-diammonium dichloro-platinum (II) (B) with hydrogen peroxide solution of concentration more than 30% at less than 30[deg]C, dissolving the product with mineral acid and precipitating with alkaline solution. Some salts and other derivatives of (A), i.e. (A,), are new compounds. An independent claim is included for new salts and other derivatives of (A), having formula (H 3N) 2Pt(OX 1)(OX 2)Cl 2 (A'). X 1, X 2calcium, magnesium, sodium, potassium, lithium, alkyl or aryl. (N.B. Compounds (A'; X 1, X 2 = alkyl or aryl) are described in the disclosure as esters (rather than ethers), and are prepared from the corresponding bases and acid anhydrides). ACTIVITY : Cytostatic. Cis-diammonium dichloro-dihydroxo-platinum (IV) disodium salt ((H 3N) 2Pt(ONa)(ONa)Cl 2) (A'') had IC 5 0 2.5 mu g/ml against SW480 (colon cancer) cells, compared with 8.2 mu g/ml for the corresponding free base. MECHANISM OF ACTION : None given in the source material.