Radiosynthesis of bromine-76 and iodine-123 labelled enantiomers of A-69024: radioligands for dopamine D1 receptor studies using PET and SPECT
| Autor: | Filomena Mattner, Vahan Papazian, Branko Dikic, Christian Loc'h, Bernard Maziere, Andrew Katsifis, Michael Kassiou |
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| Rok vydání: | 2000 |
| Předmět: |
Bicyclic molecule
Chemistry Organic Chemistry Radiosynthesis Radiochemistry Biochemistry High-performance liquid chromatography Chemical synthesis Analytical Chemistry Chiral column chromatography Drug Discovery Iodine-123 Radioligand Organic chemistry Radiology Nuclear Medicine and imaging Enantiomer Spectroscopy |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 43:339-346 |
| ISSN: | 1099-1344 0362-4803 |
| Popis: | The racemic dopamine D1 receptor antagonist A-69024 was labelled with bromine-76 for studies using PET and with iodine-123 for SPECT. [76Br]A-69024 was prepared via electrophilic bromodestannylation with NH476Br. The use of chloramine-T in acid media resulted in radiochemical yields of 70–80%. The racemic radioligand was purified by semi-preparative C-18 reverse-phase HPLC while the (+) and (−) enantiomers were separated and isolated using chiral HPLC. Average specific activities of 11 GBq/μmol were obtained. In an analogous manner, 2-[123I]A-69024 was prepared via electrophilic iododestannylation with Na123I resulting in rediochemical yields of 65–70%. Chiral HPLC gave the (+) and (−) enantiomers with specific activities of >74 GBq/μmol. The chemical and enantiomeric purity of each enantiomer of both radioligands assessed by chiral HPLC was >98%. Radiochemical purities measured by radio-TLC were >98%. The average time of synthesis for both preparations was 70 minutes. Copyright © 2000 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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