## Abstract The use of a 2‐amino‐2′‐[^18^F]fluorobenzhydrol as a radiolabelling intermediate in the synthesis of a 1,4‐benzodiazepine‐2‐one is demonstrated. 5‐Chloro‐2′‐[^18^F]fluoro‐2‐(__N__‐(2,2,2‐trifluoroethyl)amino)benzhydrol, 2, was synthesized by the coupling of the anilinodichloroborane rea
Synthesis of the benzodiazepine-1 antagonist [18F]-2-oxoquazepam
✍ Scribed by P. Johnström; T. Duelfer; S. Stone-Elander; C. Halldin; M. Haaparanta; O. Solin; J. Bergman; A. Holland; M. Steinman; G. Sedvall
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 78 KB
- Volume
- 26
- Category
- Article
- ISSN
- 0022-2135
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## 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 synthe
## Abstract A method for synthesizing ^18^F‐labelled 2‐amino‐2′‐fluorobenzhydrols under nocarrier‐added conditions for use as radiolabelled intermediates in the synthesis of[2′‐^18^F]‐1,4‐benzodiazepine‐2‐ones is presented. Anilinodichloroborane reagents were formed by the reaction of boron trichlo
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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
## Abstract Fluorine‐18 labeled 1,1‐difluoro‐2,2‐dichloroethyl aryl ethers have been prepared by a facile ^18^F‐for‐^19^F isotopic exchange reaction. The isotopic exchange proceeds in good to excellent yields (up to 85%), and is dependent on reaction time, temperature, and concentration of reactant