Concise Synthesis of Telmisartan via Decarboxylative Cross-Coupling.

[摘要]：An efficient synthesis of the angiotensin II receptor antagonist telmisartan I is presented involving a decarboxylative cross-coupling of potassium iso-Pr phthalate with 2-(4-chlorophenyl)-1,3-dioxolane 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. I is obtained in an overall yield of 35% in a convergent synthesis with the longest sequence consisting of eight steps.

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