V. Zaitsev, O. Fedorova, I. K. Mosevich
Jul 1, 2002
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Influential Citations
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Citations
Journal
Radiochemistry
Abstract
Procedures were developed for synthesis of 3,4-methylenedioxy-6-[18F]fluorobenzyl bromide I and 2-[18F]fluoro-4-methoxybenzyl bromide Ia, which are intermediates in asymmetric synthesis of fluorinated α-amino acids used in positron emission tomography (PET). The bromination procedures involving two brominating agents, an ethereal solution of HBr or triphenyldibromophosphorane in various solvents, as well as purification procedures, were compared. An optimized procedure was suggested for synthesis of I and Ia using an Anatech robotic system; the total synthesis time is 45-48 min. The radiochemical yield of I and Ia, corrected for the 18F decay, was 35-40 and 60-65%, respectively. The suggested scheme can be adapted to modern automated modules for production of radiopharmaceuticals.