A Flow-Based Synthesis of Telmisartan

A highly efficient continuous synthesis has been developed for telmisartan, the active ingredient in the antihypertensive drug, Micardis. This synthetic route employs a convergent strategy that requires no intermediate purifications or solvent exchanges. The key step in the reaction scheme is a Suzu...

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Veröffentlicht in:Journal of flow chemistry 2015-09, Vol.5 (3), p.145-147
Hauptverfasser: Martin, Alex D., Siamaki, Ali R., Belecki, Katherine, Gupton, B. Frank
Format: Artikel
Sprache:eng
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Zusammenfassung:A highly efficient continuous synthesis has been developed for telmisartan, the active ingredient in the antihypertensive drug, Micardis. This synthetic route employs a convergent strategy that requires no intermediate purifications or solvent exchanges. The key step in the reaction scheme is a Suzuki cross-coupling reaction between two functionalized benzimi-dazoles that is catalyzed by a solid-supported Pd catalyst. This flow-based approach utilizes a tubular reactor system coupled with a plug flow packed bed cartridge unit that produces telmisartan in an 81% isolated yield.
ISSN:2062-249X
2063-0212
DOI:10.1556/JFC-D-15-00002