Martin Alex D, Siamaki Ali R, Belecki Katherine, Gupton B Frank
Department of Chemistry and Department of Chemical and Life Science Engineering, Virginia Commonwealth University , Richmond, Virginia 23284, United States.
J Org Chem. 2015 Feb 6;80(3):1915-9. doi: 10.1021/jo5025333. Epub 2015 Jan 12.
A direct and efficient total synthesis has been developed for telmisartan, a widely prescribed treatment for hypertension. This approach brings together two functionalized benzimidazoles using a high-yielding Suzuki reaction that can be catalyzed by either a homogeneous palladium source or graphene-supported palladium nanoparticles. The ability to perform the cross-coupling reaction was facilitated by the regio-controlled preparation of the 2-bromo-1-methylbenzimidazole precursor. This convergent approach provides telmisartan in an overall yield of 72% while circumventing many issues associated with previously reported processes.
已开发出一种直接且高效的替米沙坦全合成方法，替米沙坦是一种广泛用于治疗高血压的药物。该方法利用高产率的铃木反应将两个功能化苯并咪唑结合在一起，该反应可由均相钯源或石墨烯负载的钯纳米颗粒催化。2-溴-1-甲基苯并咪唑前体的区域控制制备促进了交叉偶联反应的进行。这种汇聚方法以72%的总收率提供替米沙坦，同时避免了许多与先前报道的工艺相关的问题。
