4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 6, Pages 2291-2295

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.083

Keywords

[F-18]Fluoroethyltyrosine ([F-18]FET); Microfluidic technology; Positron emission tomography (PET); Small animal PET imaging

Funding

  1. Dianne and Irving Kipnes Foundation

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A new synthesis of O-(2-[F-18]fluoroethyl)-L-tyrosine [F-18]FET was developed using a NanoTek (R) 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 [F-18] fluoride. [F-18] FET was obtained after HPLC purification with 50% decay-corrected radiochemical yield starting from as little as 40 mu g 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. (C) 2012 Elsevier Ltd. All rights reserved.

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