Abstract
Electrophilic fluorination of diazepam with elemental fluorine or gas phase acetyl hypofluorite gave 3-fluorodiazepam in 20–60% yields. Nucleophilic displacement of chlorine in 3-chlorodiazepam by fluoride ion also gave 3-fluorodiazepam in modest yields (maximum: 21%). Both of these methods were used for the synthesis of 18F-labelled 3-fluorodiazepam.
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