A Fully Automated Radiosynthesis of [18F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[18F]Fluoroethyl Tosylate

被引:20
|
作者
Schoultz, Bent W. [1 ]
Reed, Brian J. [1 ,2 ]
Marton, Janos [3 ]
Willoch, Frode [2 ]
Henriksen, Gjermund [2 ,4 ]
机构
[1] Univ Oslo, Dept Chem, N-0315 Oslo, Norway
[2] Univ Oslo, Inst Basic Med Sci, N-0317 Oslo, Norway
[3] ABX GmbH, D-01454 Radeberg, Germany
[4] Norwegian Med Cyclotron Ctr, N-0424 Oslo, Norway
关键词
2-[F-18]fluoroethyl tosylate; F-18-fluoroalkylation; PET; opioid receptors; automation; solid phase extraction;
D O I
10.3390/molecules18067271
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We have developed a new method for automated production of 2-[F-18]fluoroethyl tosylate ([F-18]FETos) that enables F-18-alkylation to provide PET tracers with high chemical purity. The method is based on the removal of excess ethylene glycol bistosylate precursor by precipitation and subsequent filtration and purification of the filtrate by means of solid phase extraction cartridges (SPE). The method is integrated to a single synthesis module and thereby provides the advantage over previous methods of not requiring HPLC purification, as demonstrated by the full radiosynthesis of the potent opioid receptor PET tracer [F-18]fluoroethyldiprenorphine.
引用
收藏
页码:7271 / 7278
页数:8
相关论文
共 50 条
  • [1] Fully Automated Radiosynthesis of 1-(2-[18F]Fluoroethyl)-LTryptophan ([18F]FETrp)
    Jiang, Huailei
    Guo, Yan
    Cai, Hancheng
    Viola, Nerissa
    Shields, Anthony
    Muzik, Otto
    Juhasz, Csaba
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2023, 126 : S63 - S63
  • [2] Synthesis of high specific activity [18F]-fluoroethyl -tosylate,-spiperone, and -diprenorphine
    Carpenter, Christina
    Apana, Scott
    Berridge, Marc
    [J]. JOURNAL OF NUCLEAR MEDICINE, 2011, 52
  • [3] Synthesis and Evaluation of Three Structurally Related 18F-Labeled Orvinols of Different Intrinsic Activities: 6-O-[18F]Fluoroethyl-diprenorphine ([18F]FDPN), 6-O-[18F]Fluoroethyl-buprenorphine ([18F]FBPN), and 6-O-[18F]Fluoroethyl-phenethyl-orvinol ([18F]FPEO)
    Schoultz, Bent W.
    Hjornevik, Trine
    Reed, Brian J.
    Marton, Janos
    Coello, Christopher S.
    Willoch, Frode
    Henriksen, Gjermund
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2014, 57 (12) : 5464 - 5469
  • [4] Facile fully automated radiosynthesis and quality control of O-(2-[18F] fluoroethyl)-L-tyrosine ([18F]FET) for human brain tumor imaging
    Wang, Min
    Glick-Wilson, Barbara E.
    Zheng, Qi-Huang
    [J]. APPLIED RADIATION AND ISOTOPES, 2019, 154
  • [5] A fully automated azeotropic drying free synthesis of O-(2-[18F]fluoroethyl)L-tyrosine ([18F]FET) using tetrabutylammonium tosylate
    Orlovskaya, Victoriya
    Fedorova, Olga
    Nadporojskii, Michail
    Krasikova, Raisa
    [J]. APPLIED RADIATION AND ISOTOPES, 2019, 152 : 135 - 139
  • [6] PRODUCTION OF [18F]-FLUOROETHYLCHOLINE AND [18F]-FLUOROETHYL-L-TYROSINE IN HIGH YIELD ON AN AUTOMATED SYNCHROM SYNTHESIS MODULE
    Schmaljohann, J.
    Kuerpig, S.
    Guhlke, S.
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2009, 52 : S203 - S203
  • [7] Fully automated SPE-based synthesis and purification of 2[18F]fluoroethyl-choline for human use
    Schmaljohann, Joern
    Schirrmacher, Esther
    Waengler, Bjoern
    Waengler, Carmen
    Schirrmacher, Ralf
    Guhlke, Stefan
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2011, 38 (02) : 165 - 170
  • [8] Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane
    Bauman, A
    Piel, M
    Schirrmacher, R
    Rösch, F
    [J]. TETRAHEDRON LETTERS, 2003, 44 (51) : 9165 - 9167
  • [9] Copper-mediated reduction of 2-[18F]fluoroethyl azide to 2-[18F]fluoroethylamine
    Glaser, Matthias
    Arstad, Erik
    Gaeta, Alessandra
    Nairne, James
    Trigg, William
    Robins, Edward G.
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2012, 55 (09): : 326 - 331
  • [10] Gender dependent rate of metabolism of the opioid receptor-PET ligand [18F]fluoroethyl-diprenorphine
    Henriksen, G.
    Spilkerl, M. E.
    Sprenger, T.
    Houser, A. I.
    Platzer, S.
    Boecker, H.
    Toelle, T. R.
    Schwaiger, M.
    Wester, H. J.
    [J]. NUKLEARMEDIZIN-NUCLEAR MEDICINE, 2006, 45 (05): : 197 - 200