Concise synthesis of telmisartan via decarboxylative cross-coupling |
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Authors: | Goossen Lukas J Knauber Thomas |
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Affiliation: | Institut für Organische Chemie, TU Kaiserslautern, Erwin-Schr?dinger-Strasse, Building 54, D-67663 Kaiserslautern, Germany. goossen@chemie.uni-kl.de |
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Abstract: | An efficient synthesis of the angiotensin II receptor antagonist telmisartan is presented involving a decarboxylative cross-coupling of isopropyl phthalate (1) with 2-(4-chlorophenyl)-1,3-dioxolane (2c) as the key step (85% yield). The benzimidazole moiety is constructed regioselectively via a reductive amination-condensation sequence, replacing the previously published route via alkylation of the preformed benzimidazole. The product is obtained in an overall yield of 35% in a convergent synthesis with the longest sequence consisting of eight steps. |
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