Water → (S)-7-fluoro-12,12a-dihydro-9-oxo-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepine-1-carbonitrile

Participants

Reaction Steps

75.6 g (264 mmol) of (S)-7-fluoro-9-oxo-12,12a-dihydro-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]-benzodiazepine-1-carboxamide were suspended in 340 ml of dioxan and 45 ml of pyridine and treated dropwise at about 7° with (323 mmol) of trifluoroacetic anhydride. The reaction mixture was stirred at room temperature overnight and poured into 2 l of water. By suction filtration of the resulting suspension and drying the crystals there were obtained 45.65 g (64%) of (S)-7-fluoro-9-oxo-12,12a-dihydro-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]-benzodiazepine-1-carbonitrile, which was used in the next step without further purification.

Provenance & Evidence