N-(4,5-bis-methanesulfonyl-2-methyl-benzoyl)-guanidine, the hydrochloride thereof and method of producing thereof

摘要

Described is the hydrate of N-(4,5-bismethanesulfonyl-2 -methylbenzoyl)guanidine hydrochloride and aáprocess for its preparation in which firstly the 4-methanesulfonyl group is introduced in aáone-step reaction by reaction of the starting compound of the formula (II), in which Me is aámethyl group and Q is fluorine or chlorine, in aánucleophilic substitution with aámethanesulfinate, then in aásecond step compound of the formula (III) is converted into the acid chloride and reacted with guanidine to give N-(4,5-bismethanesulfonyl-2 -methylbenzoyl)guanidine, and in the third step by reaction in aqueous HCl is obtained hydrochloride, which is then converted into the corresponding hydrate. The hydrate of N-(4,5- bismethanesulfonyl-2-methylbenzoyl)guanidine hydrochloride may by used as an active ingredient in human and veterinary pharmaceutical preparations.