Synthesis of polymer-bound 6-mercuric carboxylate DOPA precursors and solid phase labelling method of 6-radioiodinated L-DOPA.
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.
Kawai
K
K
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
Ohta
H
H
Channing
M A
MA
Kubodera
A
A
Eckelman
W C
WC
D004295:Dihydroxyphenylalanine / Q000138:chemical synthesis*; D007457:Iodine Radioisotopes; D007980:Levodopa; D017669:Mercury Compounds / Q000138:chemical synthesis*; D011108:Polymers / Q000737:chemistry*
D007457:Iodine Radioisotopes; D017669:Mercury Compounds; D011108:Polymers; D007980:Levodopa; D004295:Dihydroxyphenylalanine