RT Journal Article
SR Electronic
T1 Facile automated synthesis of [<sup>18</sup>F]fluoromethyl-d<sub>2</sub> group in a commercial <sup>18</sup>F-synthetic module
JF Journal of Nuclear Medicine
JO J Nucl Med
FD Society of Nuclear Medicine
SP 2503
OP 2503
VO 56
IS supplement 3
A1 Byeong Min Jo
A1 Byung Seok Moon
A1 Hong Jin Lee
A1 Hyun Sik Park
A1 Byung Chul Lee
A1 Sang Eun Kim
YR 2015
UL http://jnm.snmjournals.org/content/56/supplement_3/2503.abstract
AB 2503 Objectives In our recent study, we demonstrated that 18F-fluoromethyl ether group could be used the convenient application for radiofluorination of 11C-radiotracer containing a methoxy group. For the routine application of biologically active compound, a fully automated synthesis was developed by radiofluorination of the prosthetic group (18F-CD2BrF), followed by O-alkylation in the commercially available 18F-synthetic module.Methods A TRACERlab FX N Pro chemistry module containing two reactors was used after a little modification. The position of tubing lines and valves were modified to enable for bubbling of 18F-CD2BrF into the second reactor. The flow control regulator was installed for control of bubbling rate and C18 environmental Sep-Pak cartridge was introduced for separation between CD2Br2 and 18F-CD2BrF. The air compressor line for cooling of reactor was connected with coiled copper line (1/4 inch) which was immersed the cooling bath of -50 oC. After separation of 18F-CD2BrF, we attempt the synthesis of 18F-fluoromethyl-d2 substituted PBR28 ([18F]1), TSPO selective radioligand, as previously reported by our group.Results The reactive gas-type 18F-CD2BrF was prepared from CD2Br2 with about 50% of radiolabeling yield. After distillation, the trapped 18F-CD2BrF into the second reactor was around 10% based on the initial radioactivity of fluorine-18. After alkylation of desmethyl-PBR28, the overall radiochemical yield was 5.4±0.8% (n.d.c.) with 99% of radiochemical purity. The specific activity of [18F]1 was over 266 GBq/μmol. Total automated production time needs about 80 min including HPLC purification.Conclusions A fully automated module for the introduction of 18F-fluoromethyl-d2 group was successfully developed through modifying the current module. This optimized condition could be applied to various 18F-labeled radiopharmaceuticals.