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ABSTRACT: INTRODUCTION: A novel one-pot method for preparing [(18)F]fluoromethylcholine ([(18)F]FCH) via in situ generation of [(18)F]fluoromethyl tosylate ([(18)F]FCH2OTs), and subsequent [(18)F]fluoromethylation of dimethylaminoethanol (DMAE), has been developed. METHODS: [(18)F]FCH was prepared using a GE TRACERlab FXFN, although the method should be readily adaptable to any other fluorine-(18) synthesis module. Initially ditosylmethane was fluorinated to generate [(18)F]FCH2OTs. DMAE was then added and the reaction was heated at 120°C for 10min to generate [(18)F]FCH. After this time, reaction solvent was evaporated, and the crude reaction mixture was purified by solid-phase extraction using C(18)-Plus and CM-Light Sep-Pak cartridges to provide [(18)F]FCH formulated in USP saline. The formulated product was passed through a 0.22µm filter into a sterile dose vial, and submitted for quality control testing. Total synthesis time was 1.25h from end-of-bombardment. RESULTS: Typical non-decay-corrected yields of [(18)F]FCH prepared using this method were 91mCi (7% non-decay corrected based upon ∼1.3Ci [(18)F]fluoride), and doses passed all other quality control (QC) tests. CONCLUSION: A one-pot liquid-phase synthesis of [(18)F]FCH has been developed. Doses contain extremely low levels of residual DMAE (31.6µg/10mL dose or ∼3ppm) and passed all other requisite QC testing, confirming their suitability for use in clinical imaging studies.
Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine 04/2013; 78C:26-32. · 1.09 Impact Factor
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ABSTRACT: In order to image the translocator protein (TSPO) 18kDa in the clinic using positron emission tomography (PET) imaging, we had a cause to prepare [(11)C]PBR28. In this communication we highlight our novel, recently developed, one-pot synthesis of the desmethyl-PBR28 precursor, as well as present an optimized fully automated preparation of [(11)C]PBR28 using a GE TRACERlab FX(C-Pro). Following radiolabelling, purification is achieved by HPLC and, to the best of our knowledge, the first reported example of reconstituting [(11)C]PBR28 into ethanolic saline using solid-phase extraction (SPE). This procedure is operationally simple, and provides high quality doses of [(11)C]PBR28 suitable for use in clinical PET imaging studies. Typical radiochemical yield using the optimized method is 3.6% yield (EOS, n=3), radiochemical and chemical purity are consistently >99%, and specific activities are 14,523Ci/mmol.
Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine 03/2012; 70(8):1779-83. · 1.09 Impact Factor
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ABSTRACT: The field of radiochemistry is moving towards exclusive use of automated synthesis modules for production of clinical radiopharmaceutical doses. Such a move comes with many advantages, but also presents radiochemists with the challenge of re-configuring synthesis modules for production of radiopharmaceuticals that require non-conventional radiochemistry whilst maintaining full automation. This review showcases the versatility of the Tracerlab FX(FN) synthesis module by presenting simple, fully automated methods for producing [(18)F]FLT, [(18)F]FAZA, [(18)F]MPPF, [(18)F]FEOBV, [(18)F]sodium fluoride, [(18)F]fluorocholine and [(18)F]SFB.
Journal of Labelled Compounds and Radiopharmaceuticals 05/2011; 54(6):292-307. · 0.91 Impact Factor
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ABSTRACT: As researchers explore new applications for positron emission tomography radiopharmaceuticals, the demand for effective and readily available radiopharmaceuticals continues to increase. The syntheses of two such radiopharmaceuticals, [(11)C]acetate and [(11)C]palmitate, can be automated on the GE Tracerlab FX(C-Pro) by utilizing Grignard reactions. Radiochemical purities of the [(11)C]acetate and the [(11)C]palmitate products were high (>98% and >99.9%, respectively) with average non-corrected yields of 18% (n = 3) and 10% (n = 5), respectively. These data comprise the validation trials for site qualification of clinical production of both radiopharmaceuticals.
Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine 04/2011; 69(4):691-8. · 1.09 Impact Factor
