Methylamine → HCID 54219737, compound

Participants

Reaction Steps

100 ml of methylamine (33% in ethanol) were added dropwise at 70° to a solution of 7.28 g (15.4 mmol) of (S)-2-[5-(8-oxo-10,11,12,12a-tetrahydro-8H-imidazo[5,1-c]pyrrolo[1,2-a]thieno[3,2-e][1,4]diazepin-1-yl)-1,2,4-oxadiazol-3-yl-methyl]-1,3-dihydro-isoindole-1,3-dione in 100 ml of ethanol and the mixture was stirred at 70° for a further two hours. The reaction mixture was evaporated and the residue was chromatographed (silica gel, methylene chloride/methanol 20:1). There were obtained 4.36 g (83%) of (S)-1-(3-aminomethyl-1,2,4-oxadiazol-5-yl)-10,11,12,12a-tetrahydro-8H-imidazo[5,1-c]pyrrolo[1,2-a]thieno[3,2-e][1,4]diazepin-8-one as colourless crystals of m.p. 156°-158°.

Provenance & Evidence