Das Discover PETWave eröffnet neue Reaktionswege, drastisch kürze Reaktionszeiten und höhere Ausbeuten radiochemischen Synthesen. Es eignet sich besonders vorteilhaft für die Synthesen von 11 C-, 18 F- und 68 Ga-Verbindungen.
Anthony P. Belanger, Mukesh K. Pandey, Timothy R. DeGrado, Microwave-assisted radiosynthesis of [18F]fluorinated fatty acid analogs, Nuclear Medicine and Biology, Volume 38, Issue 3, April 2011, Pages 435-441, ISSN 0969-8051,
Abstract: Microwave reactors remain largely underutilized in the field of positron emission tomography (PET) chemistry. This is particularly unfortunate since microwave synthesis elegantly addresses two of the most critical issues of PET radiochemistry with short-lived radionuclides: reaction rate and side-product formation. In this study, we investigate the efficiency of synthesis of terminally [18F]fluorinated fatty acid analogs using a commercial microwave reactor in comparison with conventional heating (CH).
The labeling precursors were methyl esters of terminally substituted alkyl bromides and iodides. Duration and temperatures of the [18F]fluorination reaction were varied. Chemical and radiochemical purities, and radiochemical yields were investigated for conventional (CH) and microwave-assisted (MW) radiosyntheses.
The results demonstrate that microwave heating enhanced [18F]fluoride incorporation to >95% (up to 55% improvement), while reducing reaction times to 2 min (∼10-fold reduction) or temperatures to 55–60°C (20°C reduction). Overall decay-corrected radiochemical yields of purified [18F]fluoro fatty acids were higher (MW=49.0±4.5%, CH=23.6±3.5%, >.05) with microwave heating and side-products were notably fewer.
Rodrigo Teodoro, Barbara Wenzel, Arata Oh-Nishi, Steffen Fischer, Dan Peters, Tetsuya Suhara, Winnie Deuther-Conrad, Peter Brust, A high-yield automated radiosynthesis of the alpha-7 nicotinic receptor radioligand [18F]NS10743, Applied Radiation and Isotopes, Volume 95, January 2015, Pages 76-84, ISSN 0969-8043,
Abstract:[18F]NS10743, a promising and highly competitive α7 nAChR radioligand has been synthesized so far by microwave irradiation using a manual single-mode device followed by a palladium-catalyzed reduction of remaining nitro-precursor for HPLC separation purposes. For further preclinical and clinical use, regulated production of [18F]NS10743 by fully automated radiosynthesis is a crucial requirement. Therefore, we chose a commercial synthesis module and developed the automated radiosynthesis of [18F]NS10743. Besides evaluation of several radiosynthesis procedures, we performed an extensive HPLC study for quantitative separation of [18F]NS10743 from the corresponding nitro precursor. After implementation of the optimized procedure on a TRACERlabTM FX F-N synthesis module, [18F]NS10743 was obtained in high radiochemical purity (≥99%) with an overall radiochemical yield of 32.2±7% (n=3). The specific activities at the end of the synthesis were 571±17 GBq/µmol (n=3).
Keywords: Alpha-7 nicotinic acetylcholine receptor radioligand; Pet WAVE microwave CEM®; Radiofluorination; Automated radiosynthesis; TRACERlabTM FX F-N
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