No-carrier-added regioselective preparation of 6-( sup 18 F)fluoro-L-dopa
- Liege Univ. (Belgium)
This paper describes the preparation of 6-({sup 18}F)fluoro-L-dopa by a no-carrier-added method based on the nucleophilic displacement of nitro groups of two commercially available substrates, 3,4-dimethoxy-2-nitrobenzaldehyde (nitroveratraldehyde) and 6-nitropiperonal. Fluorination was conducted in DMSO with fluorine-18 ({sup 18}F) in the presence of the aminopolyether Kryptofix 222 and potassium carbonate. The condensation of the fluorinated aldehydes with phenyloxazolone and the subsequent hydrolysis with HI/P yield, after purification by HPLC, only the 6-(D, L) isomers. The racemic mixture (50/50) was resolved on an analytical scale chiral column. The method, which requires 100 min (EOB) to complete, produces 6-({sup 18}F)fluoro-L-dopa with a decay-corrected radiochemical yield of 10%, an enantiomeric purity greater than 99%, and a specific activity of 1.2 Ci/mumole.
- OSTI ID:
- 6609498
- Journal Information:
- Journal of Nuclear Medicine; (USA), Journal Name: Journal of Nuclear Medicine; (USA) Vol. 31:7; ISSN 0161-5505; ISSN JNMEA
- Country of Publication:
- United States
- Language:
- English
Similar Records
Enantioselective synthesis of 6-[fluorine-18]-fluro-l-dopa from no-carrier-added fluorine-18-fluoride
High yield synthesis of 6-(/sup 18/F)fluoro-L-dopa by regioselective fluorination of protected L-dopa with (/sup 18/F)acetylhypofluorite
Related Subjects
62 RADIOLOGY AND NUCLEAR MEDICINE
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
CHEMICAL PREPARATION
CHROMATOGRAPHY
DMSO
DRUGS
FLUORINE 18
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
LIQUID COLUMN CHROMATOGRAPHY
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANIC SULFUR COMPOUNDS
RADIOISOTOPES
RADIOPHARMACEUTICALS
SEPARATION PROCESSES
SULFOXIDES
SYNTHESIS