title: Synthesis of functionalized bisphosphonates via click chemistry.
abstract: An efficient general synthetic approach giving the possibility for facile, rapid and cheap access to a wide range of novel nitrogen-bisphosphonates (N-BPs) as potent drug candidates, based on the reaction of mono- and bis-propargyl-substituted bisphosphonates with a variety of azides under Cu(i) catalysis ("click" methodology), has been developed. The method allows the incorporation of two functionalities into the N-BP molecule simultaneously, as well as to ligate in situ two N-BPs to one another via the one-pot reaction of organic dibromides with propargyl-substituted bisphosphonates, generating both the diazide and Cu(I) moieties.
authors.affiliation: Institute for Inorganic & Physical Chemistry, University of Bremen, Leobener Strasse., D-28334 Bremen, Germany.
authors.forename: Hanna
authors.initials: H
authors.lastname: Skarpos
authors.forename: Sergey N
authors.initials: SN
authors.lastname: Osipov
authors.forename: Daria V
authors.initials: DV
authors.lastname: Vorob'eva
authors.forename: Irina L
authors.initials: IL
authors.lastname: Odinets
authors.forename: Enno
authors.initials: E
authors.lastname: Lork
authors.forename: Gerd-Volker
authors.initials: GV
authors.lastname: Röschenthaler
mesh_terms: D000480:Alkynes / Q000737:chemistry; D004164:Diphosphonates / Q000138:chemical synthesis / Q000737:chemistry*; D008958:Models, Molecular; D015394:Molecular Structure
chemical_list: D000480:Alkynes; D004164:Diphosphonates