Research output: Contribution to journal › Article
A facile direct nucleophilic synthesis of O-(2-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) without HPLC purification. / Fedorova, O.; Kuznetsova, O.; Stepanova, M.; Maleev, V.; Belokon, Y.; Wester, H.-J.; Krasikova, R.
In: Journal of Radioanalytical and Nuclear Chemistry, Vol. 301, No. 2, 2014, p. 505-512.Research output: Contribution to journal › Article
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TY - JOUR
T1 - A facile direct nucleophilic synthesis of O-(2-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) without HPLC purification
AU - Fedorova, O.
AU - Kuznetsova, O.
AU - Stepanova, M.
AU - Maleev, V.
AU - Belokon, Y.
AU - Wester, H.-J.
AU - Krasikova, R.
PY - 2014
Y1 - 2014
N2 - Due to favourable in vivo characteristics, its high specificity and the longer half-life of F (109.8 min) allowing for remote-site delivery, O-(2-[F]fluoroethyl)- l-tyrosine ([F]FET) has gained increased importance for molecular imaging of cerebral tumors. Consequently, the development of simple and efficient production strategies for [F]FET could be an important step to further improve the cost-effective availability of [F]FET in the clinical environment. In the present study [F]FET was synthesized via direct nucleophilic synthesis using an earlier developed chiral precursor, the Ni complex of an alkylated ( S)-tyrosine Schiff base, Ni-( S)- BPB-( S)-Tyr-OCHCHOTs. 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]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. 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.
AB - Due to favourable in vivo characteristics, its high specificity and the longer half-life of F (109.8 min) allowing for remote-site delivery, O-(2-[F]fluoroethyl)- l-tyrosine ([F]FET) has gained increased importance for molecular imaging of cerebral tumors. Consequently, the development of simple and efficient production strategies for [F]FET could be an important step to further improve the cost-effective availability of [F]FET in the clinical environment. In the present study [F]FET was synthesized via direct nucleophilic synthesis using an earlier developed chiral precursor, the Ni complex of an alkylated ( S)-tyrosine Schiff base, Ni-( S)- BPB-( S)-Tyr-OCHCHOTs. 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]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. 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.
U2 - 10.1007/s10967-014-3121-2
DO - 10.1007/s10967-014-3121-2
M3 - Article
VL - 301
SP - 505
EP - 512
JO - Journal of Radioanalytical and Nuclear Chemistry
JF - Journal of Radioanalytical and Nuclear Chemistry
SN - 0236-5731
IS - 2
ER -
ID: 5712440