Automated synthesis of [18F]gefitinib on a modular system

被引:17
|
作者
Lappchen, Tilman [1 ]
Vlaming, Maria L. H. [2 ]
Custers, Erica [1 ]
Lub, Johan [1 ]
Sio, Charles F. [1 ]
DeGroot, Jeroen [2 ]
Steinbach, Oliver C. [1 ]
机构
[1] Philips Res Europe, Dept Biomol Engn, NL-5656 AE Eindhoven, Netherlands
[2] TNO, NL-3704 HE Zeist, Netherlands
关键词
F-18]gefitinib; Modular system; Automated synthesis; PET tracer; Imaging of drug transporters; GROWTH-FACTOR RECEPTOR; P-GLYCOPROTEIN; TUMORS; BRAIN;
D O I
10.1016/j.apradiso.2011.09.005
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
In recent years, [F-18]gefitinib PET has successfully been employed for a number of applications ranging from oncology to in vivo studies of drug transporter proteins. We here report a reliable, automated procedure for routine synthesis of this radiotracer on an Eckert and Ziegler modular system. The 3-step radiosynthesis followed by preparative HPLC-purification provided [F-18]gefitinib in 17.2 +/- 3.3% (n=22) overall decay-corrected radiochemical yield with radiochemical purity > 99% in a total synthesis time of about 2.5 h. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:205 / 209
页数:5
相关论文
共 50 条
  • [21] A practical fully automated radiosynthesis of [18F]Flurpiridaz on the module modular lab-pharmtracer without external purification
    Kurtulus Eryilmaz
    Benan Kilbas
    EJNMMI Radiopharmacy and Chemistry, 7
  • [22] A simple and efficient automated microvolume radiosynthesis of [18F]Florbetaben
    Lisova, Ksenia
    Wang, Jia
    Chao, Philip H.
    van Dam, R. Michael
    EJNMMI RADIOPHARMACY AND CHEMISTRY, 2020, 5 (01)
  • [23] How to increase the reactivity of [18F]fluoroethyl bromide:: [18F]fluoroethylation of amine, phenol and amide functional groups with [18F]FEtBr, [18F]FEtBr/NaI and [18F]FEtOTf
    Zhang, MR
    Furutsuka, K
    Yoshida, Y
    Suzuki, K
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2003, 46 (06) : 587 - 598
  • [24] A practical fully automated radiosynthesis of [18F]Flurpiridaz on the module modular lab-pharmtracer without external purification
    Eryilmaz, Kurtulus
    Kilbas, Benan
    EJNMMI RADIOPHARMACY AND CHEMISTRY, 2022, 7 (01)
  • [25] Automated synthesis of N-(2-[18F]Fluoropropionyl)-l-glutamic acid as an amino acid tracer for tumor imaging on a modified [18F]FDG synthesis module
    Liu, Shaoyu
    Sun, Aixia
    Zhang, Zhanwen
    Tang, Xiaolan
    Nie, Dahong
    Ma, Hui
    Jiang, Shende
    Tang, Ganghua
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2017, 60 (07) : 331 - 336
  • [26] Automated radiosynthesis of two 18F-labeled tracers containing 3-fluoro-2-hydroxypropyl moiety, [18F]FMISO and [18F]PM-PBB3, via [18F]epifluorohydrin
    Ohkubo, Takayuki
    Kurihara, Yusuke
    Ogawa, Masanao
    Nengaki, Nobuki
    Fujinaga, Masayuki
    Mori, Wakana
    Kumata, Katsushi
    Hanyu, Masayuki
    Furutsuka, Kenji
    Hashimoto, Hiroki
    Kawamura, Kazunori
    Zhang, Ming-Rong
    EJNMMI RADIOPHARMACY AND CHEMISTRY, 2021, 6 (01)
  • [27] The development of an automated and GMP compliant FASTlab™ Synthesis of [18F]GE-180; a radiotracer for imaging translocator protein (TSPO)
    Wickstrom, Torild
    Clarke, Alan
    Gausemel, Ingvil
    Horn, Eric
    Jorgensen, Karina
    Khan, Imtiaz
    Mantzilas, Dimitrios
    Rajanayagam, Thanushan
    in 't Veld, Dirk-Jan
    Trigg, William
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2014, 57 (01) : 42 - 48
  • [28] Improved synthesis of anti-[18F]FACBC:: improved preparation of labeling precursor and automated radiosynthesis
    McConathy, J
    Voll, RJ
    Yu, WP
    Crowe, RJ
    Goodman, MM
    APPLIED RADIATION AND ISOTOPES, 2003, 58 (06) : 657 - 666
  • [29] 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
    APPLIED RADIATION AND ISOTOPES, 2019, 152 : 135 - 139
  • [30] Simultaneous preparation of 16α-[18F]fluoroestradiol-sulphamates in an automated module.: A high-yield procedure for 16α-[18F]fluoroestradiol-17β-sulphamate
    Römer, J
    Füchtner, F
    Steinbach, J
    Kasch, H
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2001, 44 (10) : 689 - 700