149725-39-3

Upstream product

• 51522-07-7 3-methylsulphonyl-4-chlorobenzoic acid 
• 113-00-8 guanidine nitrate 
• 200423-21-8 3-methylsulfonyl-4-(1-piperidino)benzoyl chloride 
• 135051-09-1 3-methylsulfonyl-4-(1-piperidino)benzoic acid 
• 157069-50-6 4-chloro-3-(methylsulfonyl)benzoic acid methyl ester 
• 110-89-4 piperidine 

Downstream Products

• 159139-10-3 4-(4-Chlorobenzylamino)-3-methylsulfonylbenzoylguanidine hydrochloride 
• 149725-40-6 N-(3-Methanesulfonyl-4-piperidin-1-yl-benzoyl)-guanidine; compound with methanesulfonic acid 

Relevant academic research and scientific papers

Synthesis of the highly selective Na+/H+ exchange inhibitors cariporide mesilate and (3-methanesulfonyl-4-piperidino-benzoyl) guanidine methanesulfonate

The syntheses of cariporide mesilate ((4-isopropyl-3-methanesulfonyl-benzoyl) guanidine methanesulfonate, HOE 642, CAS 159138-81-5), currently being clinically investigated as a protective drug in cardiac ischemia and reperfusion states, and of HOE 694 ((3-methanesulfonyl-4-piperidino-benzoyl)guanidine methanesulfonate, CAS 149725-40-6), widely used as a physiological and pharmacological research tool in studies comprising Na+/H+ exchange (NHE) inhibition, are described. Additionally, their selectivity on the different subtypes is disclosed.

Benzoylguanidines, a process for their preparation, their use as medicaments and medicaments containing them

Benzoylguanidines of the formula I STR1 where R(1) or R(2) is equal to R(6)--S(O)n -- or R(7)R(8)N--O2 S-- and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O)n or R(7)R(8)N-- and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(7) and R(8) are equal to alkyl or phenylakyl or phenyl, and in which R(7) and R(8) may also together be a C4 -C7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system, and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(5) are together an alkylene chain, and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmics.