| abstract |
Described is a N- (4,5-bis-methanesulfonyl-2-methylbenzoyl) guanidine hydrochloride hydrate and a process for its preparation, wherein the reaction is carried out by first reacting the starting compound of formula (II) wherein Me is methyl and Q is fluorine or chlorine, in the nucleophilic substitution on the activated aromatic with methanesulfinate introduces the 4-methanesulfonyl group in a one-step reaction, in a second step the compound of formula (III) is converted to the acid chloride and reacted with guanidine to give N- (4,5-bis-methanesulfonyl) 2-methylbenzoyl) guanidine and in the third step, the reaction in aqueous hydrochloric acid affords the hydrochloride which is converted to the corresponding hydrate. N- (4,5-bis-methanesulfonyl-2-methylbenzoyl) guanidine hydrochloride hydrate can be used as an active ingredient in human and veterinary pharmaceutical preparations. |