Abstract
O-(2′-[18F]fluoroethyl)-l-tyrosine is reportedly suitable for PET-imaging of brain tumours. We report here the synthesis of Ni(II)-complex of Schiff's base (S)-[N-2-(N′-benzylprolyl)amino]-benzophenone,((S)BPB) and alkylated l-tyrosine precursor, Ni(II)-(S)-BPB-l-Tyr-O-CH2-CH2-OTs by an improved method. A fully-automated radio-synthesis including non-HPLC purification was developed with a radio-chemical yield of 24.6 ± 2% in 70 ± 2min (n = 5). Radiochemical and enantiomeric purity was > 98% and 94% respectively. Bio-distribution and micro-PET studies in C57BL/6 mice bearing B16F10 melanoma showed tumor to brain ratio of 3.36 and 3.62 respectively at 60min post-injection.
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