PURPOSE: To obtain a new benzoylguanidine and its pharmaceutically acceptable salt which are useful as medicaments for arrhythmia, myocardial infarction, angina pectoris and ischemic heart disease, and as antiatherosclerotics, agents against diabetic late complications and anti-cancer agents or the like.
CONSTITUTION: The benzoylguanidine of formula I {R(1) is R(4) R(5)N-C(X) [X is O, S or N-R(6); R(4), R(5) are each H, alkyl, alkenyl or the like, R(4) and R(5) together form methylene; R(6) is R(4) or amidine]; R(2) is H, F, Cl, Br, I, alkyl, alken-1-yl, cycloalkyl, phenyl, naphthyl, biphenylyl or the like; R(3) is H, F, Cl, Br, I, alkyl or the like}, and its pharmaceutically acceptable salt, e.g. 4-chloro-3-(N-propylcarbamoylsulfamoyl) benzoylguanidine hydrochloride, are obtained by reacting a compound of formula II (L is an eliminable group which is easily nucleophilically substituted) with guanidine.
JIYAAKU MOJIEERU
HANSUUYOOHEN RANGU
BUORUFUGANGU SHIYORUTSU
UUDOO ARUBUSU
