Microwave Accelerated Synthesis of PET Image Contrast Agents for AD Research

Ae, Kallmerten; Gb, Jones

doi:10.2174/156720510791050830

Cited by 9 publications

(1 citation statement)

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“…Realizing that microwave reactors can address the challenges of radiochemical synthesis, radiochemists have introduced microwave reactors as an alternative to conventional heating [1]. While a considerable number of articles and reviews of microwave heating have already been compiled over the past decade [2–9], space considerations and cost have inhibited this technology from widespread use. CEM (Mathews, NC) has developed a small microwave reactor system (PETWave ® ) whereby microwaves are generated outside of the hot cell and transmitted into the shielded workspace via an umbilical cord to a reaction vessel housing with a footprint of 103 cm 2 (as compared to 1480 cm 2 for CEM’s Discover ® synthetic chemistry system).…”

Section: Introductionmentioning

confidence: 99%

Microwave-assisted radiosynthesis of [18F]fluorinated fatty acid analogs

Belanger

Pandey

DeGrado

2011

Nuclear Medicine and Biology

118

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Microwave reactors remain largely underutilized in the field of 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 [ 18 F]fluorinated fatty acid analogs using a commercial microwave reactor in comparison with conventional heating.Methods-The labeling precursors were methyl esters of terminally substituted alkyl bromides and iodides. Duration and temperatures of the [ 18 F]fluorination reaction were varied. Chemical and radiochemical purities, and radiochemical yields were investigated for conventional (CH) and microwave-assisted (MW) radiosyntheses.Results-The results demonstrate that microwave heating enhanced [ 18 F]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 [ 18 F]fluoro fatty acids were higher (MW=49.0 ± 4.5%, CH=23.6 ± 3.5%, p<0.05) with microwave heating and side-products were notably fewer.Conclusion-For routine synthesis of [ 18 F]fluoro fatty acid analogs, microwave heating is faster, milder, cleaner, less variable and higher yielding than conventional heating and therefore the preferred reaction method.

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Section: Introductionmentioning

confidence: 99%