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Abstract

Procedures for the preparation of benzoyl-guanidine derivatives, of general formula (I), represented in figure 1, where: A is represented in figure 2; B represents one or more of the following groups in any desired sequence (CH2) a, (-CHOH-) b, (-CO) -c, (-CS-) d, and / or (-NR5); with a from 0 to 4, and b, c, d integers between 0 and 1; R1 represents CH3-SO2-. The procedure consists of reacting under conditions that allow nucleophilic substitution, preferably at 120 ° C under an inert gas, with a compound of the general formula R2BAQ, where Q represents a leaving group that can be substituted with the electrophile, and the resulting benzoic acid derived of the general formula (IV) represented in figure 3, it is suspended in a suitable solvent, preferably anhydrous, preferably dimethylformamide, and mixed with N-methylmorphine and carbonyldiimidazole (CDI), and combined with a mixture of a solution or suspension of a base, preferably a sodium hydride, in a suitable anhydrous solvent, preferably dimethylformamide, with a guanidine salt, preferably gunadine hydrochloride.

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