title: A new synthesis of carboxyterfenadine (fexofenadine) and its bioisosteric tetrazole analogs.
abstract: A new synthesis of carboxyterfenadine (4), based on the conversion of a alpha-halo-alkylarylketone into the corresponding substituted 2-arylalkanoic ester, is described. The enantioselective synthesis of its two bioisosteric tetrazole analogs together with preliminary biological results are reported.
authors.affiliation: Istituto di Chimica e Tecnologia del Farmaco, Università degli Studi, Perugia, Italy.
authors.forename: B
authors.initials: B
authors.lastname: Di Giacomo
authors.forename: D
authors.initials: D
authors.lastname: Coletta
authors.forename: B
authors.initials: B
authors.lastname: Natalini
authors.forename: M H
authors.initials: MH
authors.lastname: Ni
authors.forename: R
authors.initials: R
authors.lastname: Pellicciari
mesh_terms: D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D016593:Terfenadine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D006634:Histamine H1 Antagonists; D016593:Terfenadine; C093230:fexofenadine