title: Synthesis of polymer-bound 6-mercuric carboxylate DOPA precursors and solid phase labelling method of 6-radioiodinated L-DOPA.
abstract: In order to avoid separating unreacted mercury precursor and other mercury-containing compounds after the halodemercuration of a 6-mercury DOPA precursor, we developed a polymer-bound mercury precursor for the preparation of 6-halogenated DOPA. In this study, polymer-bound 6-mercuric carboxylate DOPA derivatives were synthesized from ion-exchange resin and Merrifield-type resin. Iododemercuration of polymer-bound 6-mercuric carboxylate DOPA derivatives gave higher yields (49-54%) compared with monomeric 6-mercuric trifluoroacetate protected DOPA. The radioiodination of the resin with no-carrier added iodine-125 afforded protected 6-[125I]I-L-DOPA with labelling efficiency of 92-97% with both polymer-bound 6-mercuric carboxylate DOPA derivatives.
authors.affiliation: Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Kawai
authors.forename: H
authors.initials: H
authors.lastname: Ohta
authors.forename: M A
authors.initials: MA
authors.lastname: Channing
authors.forename: A
authors.initials: A
authors.lastname: Kubodera
authors.forename: W C
authors.initials: WC
authors.lastname: Eckelman
mesh_terms: D004295:Dihydroxyphenylalanine / Q000138:chemical synthesis*; D007457:Iodine Radioisotopes; D007980:Levodopa; D017669:Mercury Compounds / Q000138:chemical synthesis*; D011108:Polymers / Q000737:chemistry*
chemical_list: D007457:Iodine Radioisotopes; D017669:Mercury Compounds; D011108:Polymers; D007980:Levodopa; D004295:Dihydroxyphenylalanine