Beilstein Journal of Organic Chemistry 2010-01-01

Efficient and improved synthesis of Telmisartan.

A Sanjeev Kumar, Samir Ghosh, G N Mehta

文献索引：Beilstein J. Org. Chem. 6 , 25, (2010)

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摘要

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.