title: A convergent approach to the total synthesis of telmisartan via a Suzuki cross-coupling reaction between two functionalized benzimidazoles.
abstract: 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.
authors.affiliation: Department of Chemistry and Department of Chemical and Life Science Engineering, Virginia Commonwealth University , Richmond, Virginia 23284, United States.
authors.forename: Alex D
authors.initials: AD
authors.lastname: Martin
authors.forename: Ali R
authors.initials: AR
authors.lastname: Siamaki
authors.forename: Katherine
authors.initials: K
authors.lastname: Belecki
authors.forename: B Frank
authors.initials: BF
authors.lastname: Gupton
mesh_terms: D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry*; D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry*; D002384:Catalysis; D003432:Cross-Linking Reagents / Q000737:chemistry*; D015394:Molecular Structure; D013237:Stereoisomerism; D000077333:Telmisartan
chemical_list: D001562:Benzimidazoles; D001565:Benzoates; D003432:Cross-Linking Reagents; D000077333:Telmisartan