A synthesis of [³H] cocaine at high specific activity

An efficient procedure is described to tritiate cocaine at high specific activity. Several tritium labelling methods were considered and evaluated against the goals of a robust synthesis employing a stable precursor, providing high radiochemical purity and specific activity [³H] cocaine of reasonable stability. Ultimately, the tritium dechlorination of a 3, 4-dichlorobenzoyl cocaine precursor became the radiolabelling method of choice. Experimental details are provided for the dichloro precursor preparation, tritium labelling as well as impure [³H] cocaine repurification.