133141-45-4Relevant academic research and scientific papers
Alkylation of azoles: Synthesis of new heterocyclic-based AT1- non-peptide angiotensin (II) receptor antagonists
Al-Azmi, Amal,George, Paulson,El-Dusouqui, Osman M. E.
, p. 515 - 520 (2007)
(Chemical Equation Presented) Several novel analogues of Losartan 2 were synthesized as potential non-peptide angiotensin (II) receptor antagonists. In these non-peptide analogues, the tetrazole and the substituted imidazole rings of Losartan 2 were replaced, respectively, by a carboxylic acid function or its methyl ester and substituted triazole, imidazole or benzimidazole moieties. The biphenyl bromide precursor 3 (BPE) used to introduce the linker between the acid/ester function and the heterocyclic moiety was synthesized using Suzuki biphenyl coupling and then incorporated into the target molecule by simple nucleophilic substitution. The fixed N-aryl isomeric forms of several azole and benzimidazole tautomers were successfully separated by HPLC using 50% aqueous acetonitrile as eluent. Intermediate reaction products and final target compounds were fully characterized spectroscopically.
