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The labelling of 2-oxoquazepam with electrophilic 18F

✍ Scribed by T. Duelfer; P. Johnström; S. Stone-Elander; A. Holland; C. Halldin; M. Haaparanta; O. Solin; J. Bergman; M. Steinman; G. Sedvall

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
585 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

2‐Oxoquazepam, 7‐chloro‐1‐(2,2,2‐trifluoroethyl)‐1,3‐dihydro‐5‐(2‐fluorophenyl)‐2H‐1,4‐benzo‐diazepine‐2‐one, is a benzodiazepine agonist. It has been shown to bind in vitro with a higher affinity to benzodiazepine type 1 receptors than to type 2 receptors. Here we report the synthesis of a trimethyltin precursor and demonstrate the feasibility of using it for radiolabelling acid‐ and base‐sensitive benzodiazepine structures such as 2‐oxoquzepam. Conversions of the electrophilic fluorine to [^18^F]‐2‐oxoquazepam on the order 20–25% were obtained.

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[2′-18F]-2-oxoquazepam: Synthesis of a 5
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Fluorination with 18F-F2 and 18F-AcOF were compared for the synthesis of 18F-fluorophenylalanines. L-phenylalanine in CF,COOH trapped 18F-AcOF more effectively than 18F-F2. The main product was ortho-18F-fluorophenylalanine when 18F-AcOF was used as a reagent. Lower radiochemical yield of 18F-fluoro