Methylamine → HCID 53887943, compound

Participants

Reaction Steps

6.01 g (12.3 mmol) of (S)-8-chloro-12,12a-dihydro-1-(3-phthalimidomethyl-1,2,4-oxadiazol-5-yl)-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepin-9-one were placed in 60 ml of ethanol and treated dropwise with 120 ml of methylamine (33% in ethanol) at 60° within 30 min. The solution was stirred at 70° for 2 hours and subsequently concentrated. By chromatography of the residue on silica gel while eluting with ethyl acetate/methanol 8/2 there were obtained 4.0 g (91%) of (S)-1-(3-aminomethyl-1,2,4-oxadiazol-5-yl)-8-chloro-12,12a-dihydro-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepin-9-one of m.p. 206°-208°.

Provenance & Evidence