A Concise and Efficient Synthesis of [2-Methyl-5-methylsulfonyl-4-(pyrrol-1-yl)benzoyl]guanidinium Methanesulfonate (Eniporide)

Autor: Baumgarth, Manfred, Gericke, Rolf
Zdroj: European Journal of Organic Chemistry; June 2000, Vol. 2000 Issue: 12 p2253-2255, 3p
Abstrakt: A new synthesis of the benzoylguanidine-type Na+/H+ antiporter inhibitor eniporide (7) is described. Starting from 2-bromo-5-fluorotoluene (1), aromatic substituents were introduced by methanesulfonylation, Pd-catalyzed carboxylation with CO, and halogen−pyrrole exchange. Guanidine acylation was performed using Mukaiyama’s procedure.
Databáze: Supplemental Index