Synthesis of [(18)F]FMISO in a flow-through microfluidic reactor: Development and clinical application

Nuclear Medicine and Biology
Ming-Qiang ZhengYiyun Huang

Abstract

The PET radiotracer [(18)F]FMISO has been used in the clinic to image hypoxia in tumors. The aim of the present study was to optimize the radiochemical parameters for the preparation of [(18)F]FMISO using a microfluidic reaction system. The main parameters evaluated were (1) precursor concentration, (2) reaction temperature, and (3) flow rate through the microfluidic reactor. Optimized conditions were then applied to the batch production of [(18)F]FMISO for clinical research use. For the determination of optimal reaction conditions within a flow-through microreactor synthesizer, 5-400 μL the precursor and dried [(18)F]fluoride solutions in acetonitrile were simultaneously pushed through the temperature-controlled reactor (60-180 °C) with defined flow rates (20-120 μL/min). Radiochemical incorporation yields to form the intermediate species were determined using radio-TLC. Hydrolysis to remove the protecting group was performed following standard vial chemistry to afford [(18)F]FMISO. Optimum reaction parameters for the microfluidic set-up were determined as follows: 4 mg/mL of precursor, 170 °C, and 100 μL/min pump rate per reactant (200 μL/min reaction overall flow rate) to prepare the radiolabeled intermediate. The optimum hy...Continue Reading

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Citations

Jun 13, 2019·Lab on a Chip·Jia WangR Michael van Dam
Sep 6, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Karla-Anne KnappH Charles Manning
Mar 10, 2018·Journal of Labelled Compounds & Radiopharmaceuticals·Ren IwataKazuhiko Yanai
Apr 15, 2017·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Olivia J KeladaDavid J Carlson
Aug 29, 2019·ACS Omega·Gulshan R Walke, Sharon Ruthstein

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