Microfluidic technology: An economical and versatile approach for the synthesis of O-(2-[18F]fluoroethyl)-l-tyrosine ([18F]FET)

• Published in: Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (6), p.2291-2295
• Main Authors: Bouvet, Vincent, Wuest, Melinda, Tam, Pui-Hang, Wang, Monica, Wuest, Frank
• Format: Article
• Language: English
• Subjects: [18F]Fluoroethyltyrosine ([18F]FET); Animals; Biological and medical sciences; Chromatography, High Pressure Liquid; Fluorine Radioisotopes; Half-Life; high performance liquid chromatography; Isotope Labeling; Medical sciences; Mice; Mice, Inbred BALB C; Microfluidic technology; Microfluidics; Neoplasm Transplantation; Neoplasms - diagnostic imaging; Pharmacology. Drug treatments; Positron emission tomography (PET); Positron-Emission Tomography; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - pharmacokinetics; screening; Small animal PET imaging; temperature; Tissue Distribution; Tyrosine - analogs & derivatives; Tyrosine - chemical synthesis; Tyrosine - pharmacokinetics
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2012.01.083

A new synthesis of O-(2-[18F]fluoroethyl)-l-tyrosine [18F]FET was developed using a NanoTek® microfluidic synthesis system. [18F]FET was obtained after HPLC purification with 50% decay-corrected radiochemical yield starting from as little as 40μg of labeling precursor. Small animal PET studies in EMT-6 tumor bearing mice showed radioactivity accumulation in the tumor (SUV60min 1.21±0.2) resulting in an increasing tumor-to-muscle ratio over time. A new synthesis of O-(2-[18F]fluoroethyl)-l-tyrosine [18F]FET was developed using a NanoTek® microfluidic synthesis system (Advion BioSciences, Inc.). Optimal reaction conditions were studied through screening different reaction parameters like temperature, flow rate, reaction time, concentration of the labeling precursor, and the applied volume ratio between the labeling precursor and [18F]fluoride. [18F]FET was obtained after HPLC purification with 50% decay-corrected radiochemical yield starting from as little as 40μg of labeling precursor. Small animal PET studies in EMT-6 tumor bearing mice showed radioactivity accumulation in the tumor (SUV60min 1.21±0.2) resulting in an slightly increasing tumor-to-muscle ratio over time.