A Successful Application of Phosphazene Base P2-tBu to [~(11)C]ABP688 Radiosynthesis in Fully Automated Synthesis Module

摘要

[~(11)C]ABP688 is the radioligand widely used for metabotropic glutamate subtype 5(mGluR5)imaging in positron emission tomography(PET).The successful production of [~(11)C]ABP688 in commercial automated synthesis module with hindered strong organic base was achieved.I compared 1,8-bis(tetramethylguanidino)naphthalene(TMGN),tert-butylimino-tri(pyrrohdino)phosphorane(BTPP),P2-tBu,P4-tBu,and NaH as a base for C-11 methylation of oxime and found P2-tBu would be a suitable alternative for the conventional inorganic bases(NaH or NaOH).Considering the GMP application,P2-tBu can provide compatibility with automated synthesizer and the resulting reliable synthesis.Three batches of the optimized condition for [~(11)C]ABP688 synthesis were examined for quality assurance.