SYNTHESIS OF N-FORMYL-3,4-DI-t-BUTOXYCARBONYLOXY-6-(TRIMETHYLSTANNYL)-L-PHENYLALANINE ETHYL ESTER AND ITS REGIOSELECTIVE RADIOFLUORODESTANNYLATION TO 6-[18F]FLUORO-L-DOPA

摘要

A protected 6-trimethylstannyl dopa derivative has been synthesized for the as a precursor for the preparation of 6-[18F]fluoro-L-dopa. The tin derivative readily reacts with electrophilic radiofluorinating agents such as [18]F2, [18F]OF2 and [18F]AcOF. The [18F]fluoro intermediate was easily hydrolyzed with HBr and the product 6-[18F]fluoro-L-dopa was isolated after HPLC purification in a maximum radiochemical yield of 23 %, ready for human use.