PROCESS FOR THE PREPARATION OF BENZAMIDINE DERIVATIVES HAVING AN ANTIMICROBIAL ACTIVITY

摘要

A process for the preparation of benzamidine derivatives corresponding to the general formula: (I) in which: - A represents a linear or branched alkyl chain containing from 3 to 9 carbon atoms; and - X represents the oxygen atom or a direct bond, with the proviso that if X represents a direct bond, the benzamidine is located in the para position relative to the alkanol group, and also pharmaceutically acceptable salts of the said derivatives; this process consists in: 1) subjecting the compound of the formula IV: (IV) in which X and A are as defined above, to catalytic hydrogenation in order to form the corresponding aniline derivatives; 2) adding sodium nitrite in an acid medium to the said aniline derivatives in order to form the corresponding diazonium compounds; 3) converting the said diazonium compounds to benzonitriles by reaction with cuprous cyanide; 4) converting the resulting benzonitrile to the compound of the formula I and 5) if appropriate, converting the said resulting compound to a pharmaceutically acceptable salt. 27 The benzamidine derivatives of formula I have antimicrobial activity and may be employed as antiseptic drugs for human or veterinary purposes, as disinfectants on inert surfaces and as preservatives.