Full Automated Synthesis of ¹¹C-β-CFT as a Dopamine Transporter Imaging Agent

To develop an automatic and efficient synthesis of ¹¹C-β-CFT as a dopamine transporter imaging agent for clinical use, ¹¹C-β-CFT was prepared from ¹¹C-Triflate-CH₃ by methylation with nor-β-CFT，and then purified by a C-18 Sep-Pak. Fully automated radiosynthesis of ¹¹C-β-CFT was carried out. The corrected radiochemical yield of ¹¹C-β-CFT was 70.2%±1.8% from ¹¹CH₃I or ¹¹CH₃Br, and the radiochemical purity was above 95%. PET imaging was performed on healthy volunteers and patients with Parkinson’s Disease (PD). PET imaging showed high radioactivity uptake of ¹¹C-β-CFT in the bilateral striatums symmetrically for the healthy volunteers, but lower radioactivity uptake in the bilateral striatums asymmetrically for the PD patients. This simple automated synthesis of ¹¹C-β-CFT is efficient with high yields, helpful with the radiation protection of personnel, and satisfactory to clinical applications.