HCID 86757686, compound → HCID 9873662, compound

Participants

Reaction Steps

450 mg of ethyl [N-[4-(4-acetimidoylhexahydro-1 H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)-methyl]sulfamoyl]acetate dihydrochloride obtained in Example 22 was dissolved in 8 ml of concentrated hydrochloric acid, and stirred at room temperature for 14 hours. The reaction mixture was evaporated, and the resulting residue was dissolved in 8 ml of concentrated hydrochloric acid, and stirred at room temperature for 4 hours. The reaction mixture was evaporated, and the resulting residue was purified through ODS column chromatography using an eluent solvent of acetonitrile/water (10/90). A small amount of 1 N hydrochloric acid was added to this, which was then freeze-dried to obtain 302 mg of [N-[4-(4-acet-imidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]sulfamoyl]acetic acid dihydro-chloride.

Provenance & Evidence