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Regioselective radiofluorodestannylation with [18F]F2 and [18F]CH3COOF: A high yield synthesis of 6-[18F]fluoro-l-dopa

✍ Scribed by Mohammad Namavari; Allyson Bishop; N. Satyamurthy; Gerald Bida; Jorge R. Barrio

Publisher
Elsevier Science
Year
1992
Weight
975 KB
Volume
43
Category
Article
ISSN
0883-2889

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✦ Synopsis

A protected 6-trimethylstannyl dopa derivative 6 has been synthesized for the first time as a precursor for the preparation of 6-[18F]fluoro-L-dopa. The tin derivative 6 readily reacted with electrophilic radiofluorinating agents such as [18F]F2 and [18F]AcOF. The [18F]fluoro intermediate 7 was easily hydrolyzed with HBr and the product 6-[18F]fluoro-L-dopa was isolated after HPLC purification in a maximum radiochemical yield of 25%, ready for human use. The various intermediates, the stannyl precursor 6 and the final product (after 18F decay) were all fully characterized by 1H, 13C, 19F and 119Sn NMR as well as high resolution mass spectroscopy.

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