ELECTROPHILIC AND NUCLEOPHILIC APROACHES TO THE SYNTHESIS OF 3-FLUORODIAZEPAM

Article abstract of DOI:10.1016/S0022-1139(00)82056-4

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