PURPOSE: To prepare an o-amino-substituted benzoylguanidine useful as a therapeutic agent for cardiovascular diseases.
CONSTITUTION: This compound is represented by formula I [R(1) is NR(50)R(6); R(2) to R(5) are each R(10)-SOa, R(11)R(12)N-CO, SR(21), F, Cl, CN or the like; R(10) to R(12) are each a 1-8C alkyl, a 3-6C alkenyl or the like; (a) is 0-4; R(21) is a CbH2b-(1-9C)-heteroaryl; (b) is 0-2], e.g. 2-amino-4-chloro-5- sulfamoylbenzoylguanidine dihydrochloride. The compound represented by the formula I is obtained by reacting a compound represented by formula II (L is a leaving group) with guanidine. The compound is useful for treating arrhythmia, cardiac infarction, cardiac ischemia, peripheral and central nervous ischemia, apoplexy, a shock state or the like. Furthermore, the compound is useful for synthesizing a medicine for surgical operation and organ transplantation and the production or the like of a scientific tool for inhibiting an Na+/H+ exchanger in diagnosis of hypertension and proliferating diseases.
HAINTSUUBUERUNAA KUREEMAN
HANSUUYOOHEN RANGU
ANDOREEASU BUAIHIERUTO
BUORUFUGANGU SHIYORUTSU
UUDOO ARUBUSU
