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Synthesis and Radiopharmaceutical Preparation of (Ethylenediamine) (1-Carbon-11-Malonate) Platinum(II) for PET Studies

State University of Ghent, Ghent, Belgium

Correspondence: For reprints contact: Bart De Spiegeleer, Dept. of Pharmaceutical Chemistry and Drug Quality Control, Faculty of Pharmaceutical Sciences, State University of Ghent, Harelbekestraat 72, B-9000 Ghent, Belgium.

ABSTRACT

Interest in the distribution, biotransformation, and mechanism of action of anticancer platinum complexes has led to the microscale, semi-automated and remote-controlled synthesis of (ethylenediamine)(1-[¹¹C]malonate) platinum(II) ([¹¹C]Ptenmal, EDMAL, JM40) from cyclotron-produced [¹¹C]cyanide. Carbon-11 cyanoacetate is produced by reacting [¹¹C]cyanide with bromoacetate. After hydrolysis, the resulting [¹¹C]malonic acid is purified and complexed to (diaquo)(ethylenediamine) platinum(II). Each step of the synthesis was optimized by studying the influence of different variables like reaction time and temperature, pH, necessary purification of intermediates, concentration and ratios of the reactants. Purification of the endproduct is achieved using preparative high performance liquid chromatography. The total incorporation of the [¹¹C]cyanide in the final product was 17–40%. After 1 hr, 40 mCi of [¹¹C]Ptenmal are produced in 10 ml sterile and isotonic dextrose solution ready for i.v. injection. The specific activity is 200 mCi/µmol at EOB.