Fully automated, high yielding production of N-succinimidyl 4-(~(18)F)fluorobenzoate ((~(18)F)SFB), and its use in microwave-enhanced radiochemical coupling reactions

摘要

A General Electric Medical Systems (GEMS) Tracerlab FX_(FN) fluorine-18 synthesis module has been reconfigured to allow rapid (45min), fully automated production of N-succinimidyl 4-[~(18)F]fluorobenzoate ([~(18)F]SFB) using the established three-step, one-pot synthesis procedure. Purification is by sep-pak only and [~(18)F]SFB is routinely obtained in 38% non-decay corrected yield, > 1 Ci/mumol specific activity, and >95% radiochemical purity (n = 20). Moreover, this report includes our preliminary research efforts into improving peptide coupling reactions with [~(18)F]SFB using microwave-enhanced radiochemistry. Reaction times can be reduced by>90%, when compared with traditional thermal reactions, with no significant effect on radiochemical reaction yield.