Hydrochloric Acid → HCID 86757690, compound

Participants

Reaction Steps

300 mg of [N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-3-fluorophenyl]-N-[(7-amidino-2-naphth-yl)methyl]sulfamoyl]acetic acid dihydrochloride obtained in Example 31 was dissolved in 10 ml of ethanol, to which was added 1 ml of a 4 N hydrochloric acid gas-dioxane solution, and stirred at room temperature for 22 hours. The reaction mixture was evaporated, and the resulting residue was dissolved in 20 ml of ethanol, to which was added 2 ml of a 4 N hydrochloric acid gas-dioxane solution, and stirred at room temperature for 7 hours. The reaction mixture was evaporated, and the resulting residue was purified through ODS column chromatography using an eluent solvent of ethanol. A s mall amount of 1 N hydrochloric acid was added to the thus-purified product, which was then freeze-dried to obtain 238 mg of ethyl [N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-3-fluorophenyl]-N-[(7-amidino-2-naphthyl)methyl]sulfamoyl]acetate dihydrochloride.

Provenance & Evidence