科研之友
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摘要
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.
- 出版日期2015-9
