A facile direct nucleophilic synthesis of O-(2-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) without HPLC purification

作者：Fedorova Olga; Kuznetsova Olga; Stepanova Maria; Maleev Victor; Belokon Yuri; Wester Hans Juergen; Krasikova Raisa^*

来源：Journal of Radioanalytical and Nuclear Chemistry, 2014, 301(2): 505-512.

DOI：10.1007/s10967-014-3121-2

• PET
• Fluorine-18
• O-(2-[F-18]fluoroethyl)-L-tyrosine
• [F-18]FET
• SPE purification

Due to favourable in vivo characteristics, its high specificity and the longer half-life of F-18 (109.8 min) allowing for remote-site delivery, O-(2-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) has gained increased importance for molecular imaging of cerebral tumors. Consequently, the development of simple and efficient production strategies for [F-18]FET could be an important step to further improve the cost-effective availability of [F-18]FET in the clinical environment. In the present study [F-18]FET was synthesized via direct nucleophilic synthesis using an earlier developed chiral precursor, the Ni-II complex of an alkylated (S)-tyrosine Schiff base, Ni-(S)-BPB-(S)-Tyr-OCH2-CH2OTs. The purification method has been developed via solid phase extraction thereby omitting cumbersome HPLC purification. The suggested SPE purification using combination of reverse phase and strong cation exchange cartridges provided [F-18]FET in high chemical, radiochemical and enantiomeric purity and 35% radiochemical yield (decay-corrected, 45 min synthesis time). The method was successfully automated using a commercially available synthesis module, Scintomics Hotbox(one). Based on the current results, the proposed production route appears to be well suited for transfer into an automated cassette-type radiosynthesizers without using HPLC.

• 出版日期2014-8