A concise synthetic route was designed for making telmisartan. The key bis-benzimidazole structure was constructed the copper-catalyzed cyclization of -haloarylamidines. By adopting this approach, telmisartan was obtained in a 7-step overall yield of 54% starting from commercially available 3-methyl-4-nitrobenzoic acid, and the use of HNO/HSO for nitration and polyphosphoric acid (PPA) for cyclization in the reported literatures were avoided.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9051534 | PMC |
| http://dx.doi.org/10.1039/d0ra00886a | DOI Listing |
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