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Merck

Efficient and improved synthesis of Telmisartan.

Beilstein journal of organic chemistry (2010-05-27)
A Sanjeev Kumar, Samir Ghosh, G N Mehta
초록

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.

MATERIALS
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Sigma-Aldrich
N-Methyl-1,2-phenylenediamine, 97%