Automated synthesis of 18F labeled 5-fluoropentyl-2-methyl-malonic acid (18F-ML-10)

TL;DRAbstract

1478 Objectives 18F-ML-10 is a member of the recently described ApoSense® family of compounds under development for the clinical radioimaging of apoptosis. Recent study reveals that 18F-ML-10 can be used as a PET imaging radiotracer for monitoring of treatment efficacy in a range of important human diseases where apoptosis is an important mechanism including myocardial infarction, cerebral stroke, and cancer. The use of automation should minimize the variance in the chemical reaction when compared with manual synthesis. Methods In order to perform preclinical and clinical studies evaluating 18F-ML-10, a simplified one-pot automated radiolabeling procedure was developed using an ML-10-mesylate precursor. The precursor was itself synthesized via t-butyl protection of 2-methylmalonic acid with isobutene, followed by introduction of the 5-hydroxypentyl group and subsequent mesylation of the alcohol. The radiolabeling procedure was performed in a remote controlled automated radiosynthesis m

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