60628-55-9

Upstream product

• 846-50-4 temazepam 
• 60628-57-1 3-fluoro-5-phenyl-7-chloro-2,3-dihydro-1H-1,4-benzodiazepin-2-one 
• 74-88-4 methyl iodide 
• 604-75-1 oxazepam 
• 963-39-3 demoxepam 
• 2888-64-4 diazepam 4-oxide 
• 60628-73-1 7-chloro-3-fluoro-1-methyl-5-phenyl-1H-1,4-benzodiazepin-2-one N⁴-oxide 
• 7719-12-2 phosphorus trichloride 
• 52395-00-3 N-methyl-N-(2-benzoyl-4-chlorophenyl)formamide 
• 10352-28-0 N-(2-benzoyl-4-chlorophenyl)formamide 
• 359-32-0 chlorofluoroacetyl chloride 
• 5606-40-6 (2-methylamino-5-chlorophenyl)-phenyl-methane-imine 
• 253-82-7 quinazoline 
• 70395-32-3 6-chloro-2-chlorofluoromethyl-1,2-dihydro-2-hydroxy-1-methyl-4-phenylquinazoline 

Relevant academic research and scientific papers

ELECTROPHILIC AND NUCLEOPHILIC APROACHES TO THE SYNTHESIS OF 3-FLUORODIAZEPAM

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.

3-FLUOROBENZODIAZEPINES

Benzodiazepines that bear a fluorine substituent in the metabolically active C-3 position were prepared by the reaction of diethylaminosulfur trifluoride (DAST) with the corresponding 3-hydroxybenzodiazepines.These products are surprisingly stable to hydrolysis and possess potent antianxiety and muscle-relaxing properties.

3-Fluorobenzodiazepines and compositions and uses thereof

3-Fluorobenzodiazepines, such as 3-fluoro-1,3-dihydro-1-methyl-7-chloro-5-phenyl-2H-1,4-benzodiazepin-2-one, useful as tranquilizers, muscle relaxants, and sedatives.

Benzophenone anti-oximes, diazepin-N-oxides, and their use as pharmaceutical agents and as intermediates for pharmaceutical agents

N-Fluorohaloacetyl-N-methylaminobenzophenone anti-oxime, the corresponding diazepin-N-oxides, their use as tranquilizers, muscle relaxants and sedatives, and their use as intermediates in the preparation of 3-fluorobenzodiazepines, which are also useful as tranquilizers, muscle relaxants and sedatives.

3-Fluorobenzodiazepines

3-Fluoro-2,3-dihydro-1H-1,4-benzodiazepin-2-ones of the formula STR1 wherein R1 is H, alkyl or fluorinated alkyl of 1-4 carbon atoms and up to 9 fluorine atoms or cycloalkylalkyl of 4-8 carbon atoms; R2 is phenyl; monohalophenyl or pyridyl; R3 is F, Cl, Br or NO2, and physiologically acceptable acid addition salts thereof, are central nervous system depressants.

Hydroxyquinazolines and their use as intermediates for pharmaceutical agents

6-Substituted-2-halofluoromethyl-1,2-dihydro-2-hydroxy-1-methyl-4-phenylquinazolines and their use as intermediates in the preparation of 3-fluorobenzodiazepines, which are useful as tranquilizers, muscle relaxants and sedatives.

Process for the preparation of 3-fluorobenzodiazepines

3-Fluorobenzodiazepines, such as 3-fluoro-1,3-dihydro-1-methyl-7-chloro-5-phenyl-2H-1,4-benzodiazepin-2-one, useful as tranquilizers, muscle relaxants, and sedatives.