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

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2291-5. doi: 10.1016/j.bmcl.2012.01.083. Epub 2012 Feb 2.

Abstract

A new synthesis of O-(2-[(18)F]fluoroethyl)-L-tyrosine [(18)F]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 [(18)F]fluoride. [(18)F]FET was obtained after HPLC purification with 50% decay-corrected radiochemical yield starting from as little as 40 μg of labeling precursor. Small animal PET studies in EMT-6 tumor bearing mice showed radioactivity accumulation in the tumor (SUV(60min) 1.21±0.2) resulting in an slightly increasing tumor-to-muscle ratio over time.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes
  • Half-Life
  • Isotope Labeling
  • Mice
  • Mice, Inbred BALB C
  • Microfluidics
  • Neoplasm Transplantation
  • Neoplasms / diagnostic imaging*
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Tissue Distribution
  • Tyrosine / analogs & derivatives*
  • Tyrosine / chemical synthesis
  • Tyrosine / pharmacokinetics

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • (18F)fluoroethyltyrosine
  • Tyrosine