PT - JOURNAL ARTICLE AU - Lionel C. Libert AU - Xavier Franci AU - Alain R. Plenevaux AU - Takashi Ooi AU - Keiji Maruoka AU - André J. Luxen AU - Christian F. Lemaire TI - Production at the Curie Level of No-Carrier-Added 6-<sup>18</sup>F-Fluoro-<span class="sc">l</span>-Dopa AID - 10.2967/jnumed.112.112284 DP - 2013 Jul 01 TA - Journal of Nuclear Medicine PG - 1154--1161 VI - 54 IP - 7 4099 - http://jnm.snmjournals.org/content/54/7/1154.short 4100 - http://jnm.snmjournals.org/content/54/7/1154.full SO - J Nucl Med2013 Jul 01; 54 AB - 6-18F-fluoro-l-dopa (18F-FDOPA) has proven to be a useful radiopharmaceutical for the evaluation of presynaptic dopaminergic function using PET. In comparison to electrophilic synthesis, the no-carrier-added (NCA) nucleophilic method has several advantages. These include much higher available activity and specific activity. Recently, we have described an NCA enantioselective synthesis using a chiral phase-transfer catalyst. However, some chemicals were difficult to implement into a commercially available synthesizer, restricting access to this radiopharmaceutical to only a few PET centers. Methods: In this paper, 2 important chemical improvements are proposed to simplify production of 18F-FDOPA, resulting in straightforward automation of the synthesis in a commercially available module. Results: First, a fast, simple, and reliable synthesis of 2-18F-fluoro-4,5-dimethoxybenzyl iodide on a solid-phase support was developed. Second, a phase-transfer catalyst alkylation of a glycine derivative at room temperature was used to enable enantioselective carbon–carbon bond formation. After hydrolysis and high-performance liquid chromatography purification, a high enantiomeric excess of 18F-FDOPA (∼97%) was obtained using a chiral catalyst available from a biphenyl 3 substrate. The total synthesis time was 63 min, and the decay-corrected radiochemical yield was 36% ± 3% (n = 8). Conclusion: By exploiting the advantages of this NCA approach, using a starting activity of 185 GBq of NCA 18F-fluoride, high activities of 18F-FDOPA (&gt;45 GBq) with high specific activity (≥753 GBq/μmol) are now available at the end of synthesis for use in clinical investigations.