PURPOSE: To obtain a compound having platelet aggregation action as an orally administrable GPIIb/IIIa receptor antagonist and useful as a medicine such as an improver of ischemic heart disease or an adjuvant in operation of cardiac surgery or vascular surgery.
CONSTITUTION: This benzamidine derivative is expressed by formula I [R1 and R2 are each H or an ester residue; X1 is an alkylene; X2 is a single bond or an alkylene; (m) is 0, 1 or 2; (n) is 0 or 1, with the proviso that when (m) is 0, (n) is 1], e.g. 4-[4-(4-amidinophenyl)-1-piperazinyl]-1,3-piperidinediacetic acid. The compound of formula I is obtained by reacting a nitrile compound expressed by formula II with an alcohol each as methanol or ethanol in the presence of chlorine gas at -40 to 0°C to imidate the nitrile compound and reacting the imidated compound with an amine such as ammonia or an amine salt such as ammonium carbonate. The compound of formula I is excellent in persistency of action and has low toxicity.
MATSUMOTO YUZO (JP)
ICHIHARA MASATO (JP)
KAWASAKI TOMIHISA (JP)
KAKO SEIJI (JP)
YANAGISAWA ISAO (JP)
