New synthesis of fluorine-18-labeled 6-fluoro-L-dopa by cleaving the carbon-silicon bond with fluorine
A new synthesis of 3,4-dihydroxy-6-( YF)fluoro-L-phenylalanine using 6-trimethylsilyl-3,4-dimethoxy-L-dopa-ethylester as a fluorination substrate is described. The silane is prepared from the corresponding bromo compound by reacting the latter with magnesium and trimethylsilyl chloride. Reaction of the silane with ( YF)F2 in a mixture of freon-11/CCl4 (1:1) kept in a dry ice bath, subsequent hydrolysis with concentrated HBr in a bath at 140 degrees C, and simple chromatographic purification yielded YF-labeled 6-fluoro-L-dopa. A radiochemical yield of about 8% was achieved at the end of the 1-hr synthesis. The specific activity at the end of the synthesis was about 680 mCi/mmol after a 30-min irradiation.
- OSTI ID:
- 6302766
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 11
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
CHEMICAL REACTION YIELD
DOPA
FLUORINE 18
SILANES
AMINO ACIDS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
CARBOXYLIC ACIDS
DRUGS
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
HYDRIDES
HYDROGEN COMPOUNDS
HYDROXY ACIDS
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
NEUROREGULATORS
NUCLEI
ODD-ODD NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC SILICON COMPOUNDS
RADIOISOTOPES
SILICON COMPOUNDS
SYNTHESIS
YIELDS
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials