Optimization of the preparation conditions of radioiodoepidepride: A dopamine D2receptor antagonist radioligand

The synthesis of dopaminergic radioligands labelled with tritium and iodine‐125

“…81 Also, several benzamide class dopaminergics have been radioiodinated using this versatile methodology as well. [82][83][84][85][86] Although early in this discussion it was mentioned that the relatively small size of dopaminergic substrates usually ruled out the use of most added bulky radiolabelled appendages like the Bolton-Hunter reagent, one prosthetic group that has been successfully employed for radioiodinations is the vinylstannyl group. This labelling option has been exceptionally valuable in preparing target compounds that required radioiodination in positions other than aromatic rings.…”

Radiochemistry and radiopharmaceuticals

“…It has been used recently to make labelled lanreotide, 170 cannabinergic indole analogues, 171 9-aminoacridine derivatives, 172 5-iodo-2 0 -deoxyuridine, 173 O-6-3-iodobenyl-2 0 -deoxyguanosine, 174 some iodobenzylguanidine analogues, 175 4-fluorophe-nyl{1-[2-(4-iodophenyl)ethyl]piperidin-4-yl} methanone, 176 2-(4-iodophenylamino) pyrido [2,3-d]pyrimidin-7-one, 177 iodometomidate 178 and 2-(4 0 -iodo-biphenyl-4sulfonylamino)-3-methyl-butyramide. 179 Another widely used method of electrophilic substitutuion by radioiodine is to use oxidising reagents such as chloramine-T; this method has been used to label iodoepidepride, 180 5-chloro-7-iodo-8-hydroxyquinoline 181 and indomethacin 182 as well as radioiodinated azide and isothiocyanate derivatives of cocaine. 183 [ 125 I]-iodoberberine 184 and N-[3-(4-morphilino)propyl]-Nmethyl-2-hydroxy-5-[ 125 I]iodo-3-methyl-benzylamine 185 have both been labelled by nucleophilic exchange with radioiodide anions.…”