HCID 54418996, compound → HCID 54050108, compound

Participants

Reaction Steps

1 g (2.2 mmol) of (S)-1-(3-diallylaminomethyl-1,2,4-oxadiazol-5-yl)-7-fluoro-12,12a-dihydro-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepin-9-one in 5 ml of methanol were hydrogenated at room temperature and normal pressure in the presence of 22 mg of 5% palladium-on-charcoal. After separating the catalyst the residue was purified by chromatography on silica gel while eluting with ethyl acetate/hexane/triethylamine 17/2/1. There was obtained 0.53 g (56%) of (S)-7-fluoro-12,12a-dihydro-1-(3-di-n-propylaminomethyl-1,2,4-oxadiazol-5-yl)-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepin-9-one (oil: Rf. 0.36; Kieselgel 60 F254. Eluent: ethyl acetate/hexane/triethylamine 17/2/1), which was converted into the hydrochloride.

Provenance & Evidence