| Autor: |
Krasikova, R. N., Kuznetsova, O. F., Fedorova, O. S., Mosevich, I. K., Maleev, V. I., Belokon, Yu. N., Savel’eva, T. F., Sagiyan, A. S., Dadayan, S. A., Petrosyan, A. A. |
| Předmět: |
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| Zdroj: |
Radiochemistry; Sep2007, Vol. 49 Issue 5, p512-518, 7p, 4 Diagrams, 1 Chart |
| Abstrakt: |
A new procedure was suggested for asymmetric synthesis of of 6-[18F]fluoro-3,4- L-dihydroxyphenylalanine (6-18F- L-FDOPA), an important radiotracer for studies of the dopaminergic system by positron emission tomography (PET). The key step of the synthesis is stochiometric asymmetric alkylation of chiral Ni(II) complexes using 3,4-methylenedioxy-6-[18F]fluorobenzyl bromide as alkylating agent. A series of Ni(II) complexes containing various substituents in the benzyl group were tested. The highest enantiomeric purity of 6-18F- L-FDOPA was attained with the complex derived from ( S)- N-(2-benzoylphenyl)-1-(3,4-dichlorobenzyl)-pyrrolidine-2-carboxamide, Ni-DCBPB-Gly, under mild alkylation conditions (CH2Cl2, 40°C, potassium tert-butylate as base). Such conditions are favorable from the viewpoint of synthesis automation. The radiochemical yield of 6-18F- L-FDOPA corrected for the radioactive decay was 10–15% at a synthesis time of 120 min, including purification by semipreparative HPLC. The radiochemical and chemical purity of the product exceeded 99%, and the enantiomeric purity was as high as 95%, meeting the requirements for using 6-18F- L-FDOPA in PET practice. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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