Literature DB >> 27314451

Automated and efficient radiosynthesis of [(18)F]FLT using a low amount of precursor.

Patrice Marchand1, Ali Ouadi2, Michel Pellicioli3, Jacky Schuler4, Patrice Laquerriere5, Frédéric Boisson6, David Brasse7.   

Abstract

INTRODUCTION: Since 1991 until now, many radiosyntheses of [(18)F]FLT have been published. Most of them suffer from side reactions and/or difficult purification related to the large amount of precursor necessary for the labeling step. A fully automated synthesis using only commercial and unmodified materials with a reduced amount of precursor would be desirable.
METHODS: We first explored the possibility to elute efficiently [(18)F]fluorine from commercial and unmodified cartridges with various amount of base. Based on these results, 10mg and 5mg of precursors were used for the fluorination step. The best conditions were transposed in an automated process for a one pot two steps synthesis of labeled FLT.
RESULTS: Using commercial and non-treated carbonate form of QMA cartridges, we were able to elute quantitatively the [(18)F]fluorine with a very low amount of base (0.59mg) and, with only 5mg of precursor, to perform an efficient fluorination reaction with up to 94% incorporation of [(18)F]fluorine. The synthesis was fully automated and radiochemical yields of 54% (decay corrected) were obtained within a synthesis time of 52minutes.
CONCLUSION: We demonstrate that a fully automated and efficient radiosynthesis of [(18)F]FLT is feasible with only 5mg of precursor. Compare to the present state of the art, our method provides high yields of pure [(18)F]FLT and is broadly adaptable to other synthesis automates.
Copyright © 2016 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Automated synthesis; FLT (3′-deoxy-3′-[(18)F]-fluoro-thymidine); Hindered alcohol; Preclinical

Mesh:

Substances:

Year:  2016        PMID: 27314451     DOI: 10.1016/j.nucmedbio.2016.05.009

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN: 0969-8051            Impact factor:   2.408


  4 in total

1.  Integration of High-Resolution Radiation Detector for Hybrid Microchip Electrophoresis.

Authors:  Jason Jones; Noel S Ha; Alec G Barajas; Arion F Chatziioannou; R Michael van Dam
Journal:  Anal Chem       Date:  2020-02-07       Impact factor: 6.986

2.  Production of diverse PET probes with limited resources: 24 18F-labeled compounds prepared with a single radiosynthesizer.

Authors:  Jeffrey Collins; Christopher M Waldmann; Christopher Drake; Roger Slavik; Noel S Ha; Maxim Sergeev; Mark Lazari; Bin Shen; Frederick T Chin; Melissa Moore; Saman Sadeghi; Michael E Phelps; Jennifer M Murphy; R Michael van Dam
Journal:  Proc Natl Acad Sci U S A       Date:  2017-10-10       Impact factor: 11.205

3.  Comparison of the [18F]-FDG and [18F]-FLT PET Tracers in the Evaluation of the Preclinical Proton Therapy Response in Hepatocellular Carcinoma.

Authors:  David Brasse; Hélène Burckel; Patrice Marchand; Marc Rousseau; Ali Ouadi; Marie Vanstalle; Christian Finck; Patrice Laquerriere; Frédéric Boisson
Journal:  Mol Imaging Biol       Date:  2021-04-13       Impact factor: 3.488

4.  3'-[18F]fluoro-3'-deoxythymidine ([18F]FLT) Positron Emission Tomography as an In Vivo Biomarker of inhibition of CDK 4/6-Rb pathway by Palbociclib in a patient derived bladder tumor.

Authors:  James L Tatum; Joseph D Kalen; Paula M Jacobs; Lisa A Riffle; Amy James; Lai Thang; Chelsea Sanders; Melinda G Hollingshead; Falguni Basuli; Jianfeng Shi; James H Doroshow
Journal:  J Transl Med       Date:  2022-08-18       Impact factor: 8.440

  4 in total

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