Acetic Acid Mediated Electrochemical Synthesis of Benzazole and its Application in the Synthesis of Pharmaceutically Active Compounds

Abstract

An acetic acid promoted electrochemical synthesis of benzazoles, benzimidazoles, benzthiazoles and benzoxazoles, is reported. The method offers large substrate scope, good functional group tolerance, while using cheap electrolyte. The method uses acetic acid as the electrolyte which has a better solubility in methanol, hence the reaction time is less and product formation is observed in high yield without much side product. This electrochemical method is further utilised to synthesise thiabendazole, fuberidazole, chlormidazole and advance intermediates of bilastine and clemizole in good yields.

Synthesis, crystal structure, DFT calculation and Hirshfeld surface analysis of N-(4-methyl phenyl)-2-(3-nitro-benzamido) benzamide

“…It was heated, the solid product was collected within one minute [11]. The product was filtered out, and recrystallized from ethanol, to obtain a high-quality crystal, the bis amide was dissolved in acetic acid and let for 6 1).…”

“…Amides are important functional groups in biochemical and pharmacological processes, and are widely used as building blocks for the synthesis of other compounds [6]. The ring opening reaction to form amides involves the cleavage of a cyclic structure, such as a lactam or a cyclic imide, and the formation of an amide bond between an amino group and a carbonyl group.…”

Facile Synthesis of Benzimidazoles via Oxidative Cyclization of Acyclic Monoterpene Aldehyde with Diamines: Studies on Antimicrobial and in Vivo Evaluation of Zebrafish

“…Two‐nitrogen benzimidazole is also a significant pharmacophore in this context. Various benzimidazole compounds have achieved clinical approval, such as albendazole, mebendazole, and thiabendazole, [10a–b] in addition to the anticancer advantages associated with benzimidazole. The presence of carbendazim [ 11a – b ] and fuberidazole in the novel benzimidazoles increases the likelihood that they may also demonstrate significant biological activity Figure 1.…”