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Fully automated synthesis of O-(2′-[18F]fluoroethyl)-l-tyrosine ([18F]FET) using solid phase extraction (SPE) purification with neutral alumina

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Abstract

[18F]FET was synthesized using O-(2′-tosyloxyethyl)-N-trityl-l-tyrosine-tert-butyl ester (TET) precursor. SPE purification of [18F]FET, after radio-synthesis, using neutral alumina column was satisfactory, with radiochemical and enantiomeric purity of >99 %. Decay-uncorrected synthesis yield with 8 mg TET was 19.07 ± 1.3 and 8.76 ± 0.46 % when eluted in 35 and 17 mL of buffered saline, respectively, for practical considerations. O-(2′-hydroxyethyl)-l-tyrosine formed during synthesis could be reduced nine-fold to <2 µg/mL by using 2 mg TET but with ~30 % less yield. Bio-distribution and Micro-PET imaging in C57BL/6 mice with B16F10-induced-melanoma showed tumor/brain ratio of 2.8 at 60 min. With SPE, [18F]FET production is simplified like 2-[18F]FDG.

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Acknowledgments

Our sincere thanks to cyclotron staffs of the Medical Cyclotron Facility, Radiation Medicine Centre, BARC, Mumbai for providing radioactivity as per our requirements for our experiments Our special thanks to Dr. B. L. Malpani, Radiation Medicine Centre, BARC, Mumbai for providing Rabbit PET/CT images and to Mr. Arpit Mitra, BRIT, for carrying out the sterility and BET tests.

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Correspondence to M. G. R. Rajan.

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Lakshminarayanan, N., Kumar, A., Roy, S. et al. Fully automated synthesis of O-(2′-[18F]fluoroethyl)-l-tyrosine ([18F]FET) using solid phase extraction (SPE) purification with neutral alumina. J Radioanal Nucl Chem 310, 991–999 (2016). https://doi.org/10.1007/s10967-016-4900-8

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