Abstract
[F-18]FBAM, a thiol reactive bifunctional agent, was successfully synthesized using continuous flow chemistry in a micro reactor that is part of Advion NanoTek Micro-fluidic Synthesizer. As the radiofluorination was carried out microfluidically, a very small amount of precursor was used and over all radiochemical yield was 38% ± 4% (n = 8, decay corrected) and the radiochemical purity was ≥98% with specific activity of 430 mC/μmol. The total reaction time including HPLC purification was 55 min that is 14 min more than manual synthesis and 6 min less than fully automated synthesis.
Highlights
Bioactive peptides and proteins are important key regulators in cell growth and cellular functions in living organisms [1]-[3]
We treated maleimide 8 with either NaH or K2CO3 in THF or DMF at room temperature followed by the addition of 1,6-dibromohexane, 9; after, stirring the reaction mixture at reflux only trace amounts of the desired product 11 were produced
It is possible that the N-Alkylation of maleimide does not proceed as expected because the maleimide anion underwent a 1,4-addition to another molecule of maleimide instead of reacting with alkyl bromide
Summary
Bioactive peptides and proteins are important key regulators in cell growth and cellular functions in living organisms [1]-[3]. Harsh reaction conditions required to directly radiofluorinate these sensitive biomolecules hampered the preparation of the requisite tracers in good yields and high specific activity To address these problems, radiochemists have taken advantage of bifunctional agents, known as prosthetic groups. Microfluidics represents a useful approach to conduct the reactions with minimal quantities of expensive precursors; other advantages include reduced reaction times and increased radiolabeling yields These effects are realized due to the high surface to volume ratio encountered while the reagents are flowing through the microchannel which is accompanied by rapid mixing of the reagents leading to increased heat transfer between the reactants. One of the commercially available microfluidic devices with micro-channel system (MCS) is the Advion NanoTek Microfluidic Synthesizer This unit consists of three modules called the reagent, reactor and concentrator modules. We wish to report an improved synthesis of [18F] FBAM utilizing this microfluidic system involving continuous flow
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