A Flow-based Synthesis of Telmisartan

    Alex Martin, Ali Siamaki, Katherine Belecki, B. Gupton

    • Department of Chemistry and Department of Chemical and Life Science Engineering Virginia Commonwealth University 601 W. Main St. Richmond Virginia 23284 United States

    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 benzimidazoles 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.

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