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1. Automated commercial synthesis system for preparation of O-(2-[18F]fluoroethyl)-L-tyrosine by direct nucleophilic displacement on a resin column

Author

Ganghua Tang, Zuhan Huang, Xiaolan Tang, Lei Luo, Mingfang Wang, and Manquan Gan

Subjects
Chemistry, Organic Chemistry, Biochemistry, Chemical synthesis, Analytical Chemistry, chemistry.chemical_compound, Nucleophile, Yield (chemistry), Drug Discovery, Organic chemistry, Radiology, Nuclear Medicine and imaging, Ion-exchange resin, Synthesis system, Fluoride, Spectroscopy, Fluoroethyl, Nuclear chemistry, Decay correct
Abstract

A slightly modified automated commercial synthesis system for preparation of O-(2-[18F]fluoroethyl)-l-tyrosine (FET), an amino acid tracer for tumor imaging with positron emission tomography, is described. Direct nucleophilic fluorination of [18F]fluoride with 1,2-di(4-methylphenylsulfonyloxy)ethane on a quaternary 4-(4-methylpiperidinyl)-pyridinium functionalized polystyrene anion exchange resin gave 1-[18F]-2-(4-methylphenylsulfonyloxy)ethane, then [18F]fluoroalkylation of l-tyrosine yielded FET. The overall radiochemical yield with no decay correction was about 8–10%, the whole synthesis time was about 52 min, and the radiochemical purity was above 95%. Copyright © 2003 John Wiley & Sons, Ltd.

Published
2003

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