S. Wyrick, S. Chaney
Apr 1, 1988
Citations
0
Influential Citations
31
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
Cis-diamminedichloroplatinum (II) (cisplatin) is one of the most widely used anticancer drugs today. However, platinum compounds possessing the 1,2-diaminocyclohexane (DACH) carrier ligand offer advantages over cisplatin with regard to bioavailability, activity and decreased renal toxicity. The trans-(d,1)-1,2-diaminocyclohexane derivatives are the isomeric forms recently chosen by the NCI for large animal studies and phase I/II clinical trials. Here we report the synthesis of four trans-(d,1)-1,2-diaminocyclo-hexane platinum derivatives labeled with tritium in the cyclohexane ring by catalytic reduction of a cyclohexene precursor with carrier-free tritium gas over 10% Pd/C.