Abstract
We describe the synthesis of 2′-[ 18F]fluoroflumazenil (FFMZ), which differs from the typically used [ 18F]fluoroethylflumazenil (FEFMZ) for benzodiazepine receptor imaging. For one-pot one-step labeling, the precursors, 2′-tosyloxyflumazenil (TFMZ) and 2′-mesyloxyflumazenil (MFMZ), were synthesized in three steps. The precursors were successfully labeled with no-carrier-added 18F-fluoride which was activated by repeated azeotropic distillation with Kryptofix 2.2.2./potassium carbonate in MeCN. An automated system for labeling and purification of [ 18F]FFMZ was developed. Labeling efficiency and radiochemical purity of [ 18F]FFMZ after synthesis by the automated system were 68% and 98%, respectively. Specific binding of [ 18F]FFMZ to central benzodiazepine receptor of rats was demonstrated by phosphoimaging.
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