Alkylation of Azoles: Synthesis of New Heterocyclic‐Based AT₁‐Non‐Peptide Angiotensin (II) Receptor Antagonists.

Abstract

Antagonists. -Analogues of losartan, the most successful antagonist in antihypertensive therapy, are synthesized by replacing the tetrazole and the imidazole rings with a carboxylic acid function or its methyl ester and substituted triazole, imidazole or benzimidazole moieties. -(AL-AZMI*, A.; GEORGE, P.; EL-DUSOUQUI, O. M. E.; J. Heterocycl. Chem. 44 (2007) 3, 515-520; Dep. Chem., Fac. Sci., Univ. Kuwait, Safat 13060, Kuwait; Eng.) -H. Hoennerscheid 40-220

Transition-Metal-Free and Base-Free Electrosynthesis of 1H-Substituted Benzimidazoles

“…The 1Hsubstituted benzimidazole derivatives are traditionally prepared through either reductive amination 8 or through deprotonation followed by nucleophilic substitution with carbon electrophiles. 9,10 For the deprotonation synthetic route, the weak acidity of the NH group can necessitate the use of strong bases and elevated reaction temperatures. These harsh conditions can lead to particularly challenging preparations of benzimidazole derivatives that contain base-sensitive functionalities.…”