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.
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