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A microwave-assisted synthesis of cisplatin, cis-[Pt(NH3)2Cl2], has been developed and optimized on both a 0.2 and 0.05 millimolar scale. The optimized synthetic procedure was modeled after the Lebedinskii-Golovnya method and is suitable for incorporating the radionuclide, Pt, into cisplatin for biological studies. Highest yields (47 %) and purity are obtained using a K2PtCl4:NH4OAc:KCl molar ratio of 1:4:2 at a temperature of 100 ̊C. The entire synthesis and purification procedure requires approximately 80 min. At a reaction temperature of 150 ̊C, the trans isomer is the exclusive product, suggesting that complexes of the general form, trans-[Pt(RNH2)2Cl2], can be synthesized directly from K2PtCl4 using [RNH3]OAc (R = alkyl or aryl moieties) via a microwave process. Two novel separation procedures have been developed which efficiently remove the major impurity (1:1 Magnus-type salt) from the crude reaction product, yielding a product of purity comparable to that obtained by the Dhara method and suitable for biological studies. These procedures are applicable to both the micro and macro scale of synthesis. The question of whether this microwave-assisted synthesis of cisplatin will be a preferred method for incorporating Pt into cisplatin is yet to be determined. Page 1 of 23 Dalton Transactions D al to n Tr an sa ct io ns A cc ep te d M an us cr ip t