Efficient and improved synthesis of Telmisartan.
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Kumar AS, Ghosh S, Mehta GN
Efficient and improved synthesis of Telmisartan.
Beilstein J Org Chem. 2010 Mar 11;6:25. doi: 10.3762/bjoc.6.25.
- PubMed ID
- 20502601 [ View in PubMed]
- Abstract
An efficient synthesis of the angiotensin II receptor antagonist Telmisartan (1) is presented involving a cross coupling of 4-formylphenylboronic acid 10 with 2-(2-bromophenyl)-4,4-dimethyl-2-oxazoline (11) as the key step (90% yield). The benzimidazole moiety 15 was constructed regioselectively via a reductive amination-condensation sequence, replacing the alkylation of the preformed benzimidazole step in the previously published route. This methodology overcomes many of drawbacks associated with previously reported syntheses.