TY - JOUR T1 - Multi-step, remote synthesis of 6-[<sup>18</sup>F]fluorodopamine via nucleophilic aromatic substitution JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 1481 LP - 1481 VL - 53 IS - supplement 1 AU - Amy Vavere AU - Yu-Shin Ding AU - Scott Snyder Y1 - 2012/05/01 UR - http://jnm.snmjournals.org/content/53/supplement_1/1481.abstract N2 - 1481 Objectives 6-[18F]fluorodopamine ([18F]FDA) is a catecholamine that is actively taken into cells via norepinephrine transporters and is useful in PET imaging of pheochromocytomas and other neuroendocrine tumors. We sought to develop and optimize a method for remote, routine production of [18F]FDA for clinical research by nucleophilic aromatic substitution with 18F-. Methods Using a PETChem Solutions, Inc. remote synthesis module, [18F]FDA was prepared via modification of the method of Ding, et al {1991}. Aqueous 18F- was trapped on QMA, removed with Kryptofix 2.2.2/K2CO3 in CH3CN and H2O, and dried. 6-Nitropiperonal was fluorinated in DMSO at 120°C for 10 min and transferred onto a C-18 SepPak after dilution in water and passage through an alumina cartridge. 6-[18F]Fluoropiperonal was eluted with CH2Cl2 and sent to a second reactor where all remaining steps occurred. After evaporation of solvent, nitropropene was formed by addition of 6:1 CH3NO2/acetic acid and heating to 100°. Solvent was again evaporated followed by reduction with LAH/THF and removal of THF. [18F]FDA was formed by deprotection of the catechol with HI at 160° and diluted in phosphate buffer. Filtration (0.22 µm) to remove aluminate salts and semi-prep HPLC on a C-18 column yielded purified [18F]FDA in 9 minutes. RP-HPLC was used to determine radiochemical purity of the final product. Results Final, radiochemical yield of purified [18F]FDA (not optimized) was 4% (corrected to EOB) with an overall synthesis time of 2 hours. Radiochemical purity was 96% resulting in 3 mCi of final product (prior to reformulation) starting from 200 mCi. Conclusions While optimization is still ongoing, we succeeded in developing a method for the remote, nucleophilic production of [18F]FDA. Even with lower yield than previously reported, this synthesis is easily capable of producing enough activity for a single patient (5-10 mCi), when scaled up. Further optimization, reformulation, and quality control studies are underway ER -