Facile Synthesis of Benzimidazoles via N‑Arylamidoxime Cyclization

A facile synthesis of benzimidazoles was described by a one-pot process containing acylation–cyclization of N-arylamidoxime. This method provided an alternative synthesis of benzimidazoles with a certain diversity of substituted groups in acceptable yields (up to 96%). More importantly, the construc...

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Veröffentlicht in:ACS omega 2022-12, Vol.7 (49), p.45678-45687
Hauptverfasser: Qin, Hongjian, Odilov, Abdullajon, Bonku, Emmanuel Mintah, Zhu, Fuqiang, Hu, Tianwen, Liu, He, Aisa, Haji A., Shen, Jingshan
Format: Artikel
Sprache:eng
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Zusammenfassung:A facile synthesis of benzimidazoles was described by a one-pot process containing acylation–cyclization of N-arylamidoxime. This method provided an alternative synthesis of benzimidazoles with a certain diversity of substituted groups in acceptable yields (up to 96%). More importantly, the construction of bis-benzimidazole (8), the key intermediate for making telmisartan, was achieved by adopting this method that enabled avoiding the undesired nitration with nitric/sulfuric acid and the cyclization in polyphosphoric acid in the existing operations.
ISSN:2470-1343
2470-1343
DOI:10.1021/acsomega.2c06554