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Title:
PRODUCTION METHOD FOR RADIOLABELED ARYL COMPOUND
Document Type and Number:
WIPO Patent Application WO/2019/027059
Kind Code:
A1
Abstract:
The purpose of the present invention is to produce a radiolabeled aryl compound by a simple method in which labeling can be carried out in a short time in high radiochemical yield and which renders the radiolabeled aryl compound usable in formulation immediately after the labeling. The present invention relates to a production method for a radiolabeled aryl compound (I), characterized by reacting an arylboronic acid compound (II) with a radioactive nuclide selected from among 211At, 210At, 123I, 124I, 125I, and 131I in water in the presence of an oxidant selected from among alkali metal iodides, alkali metal bromides, N-bromosuccinimide, N-chlorosuccinimide, and hydrogen peroxide. (In the formulae, the symbols are as defined in the description.)

Inventors:
SHIRAKAMI YOSHIFUMI (JP)
IKEDA HAYATO (JP)
KANAI YASUKAZU (JP)
SHIMOSEGAWA EKU (JP)
HATAZAWA JUN (JP)
WATABE TADASHI (JP)
KANEDA KAZUKO (JP)
Application Number:
PCT/JP2018/030006
Publication Date:
February 07, 2019
Filing Date:
August 03, 2018
Export Citation:
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Assignee:
UNIV OSAKA (JP)
International Classes:
C07F13/00; C07B59/00
Domestic Patent References:
WO2007079953A22007-07-19
Foreign References:
JP2009521469A2009-06-04
US4826672A1989-05-02
US5077035A1991-12-31
JP2001503412A2001-03-13
JP2009521469A2009-06-04
JP2017151632A2017-08-31
Other References:
KABALKA, G. W. ET AL.: " "Synthesis of iodine-125 labeled 3- quinuclidinyl 4'-iodobenzilate", NTERNATIONAL JOURNAL OF RADIATION APPLICATIONS ANDINSTRUMENTATION PART B: NUCLEAR MEDICINE AND BIOLOGY, vol. 16, no. 4, 1 January 1989 (1989-01-01), pages 359 - 360, XP023085484, ISSN: 0883-2897, DOI: 10.1016/0883-2897(89)90099-8
J'VLEYER, G. J. ET AL: "Synthesis and analysis of 2-[211At]-L- phenylalanine and 4-[211At]-L-phenylalanine and their uptake in human glioma cell cultures in-vitro", APPLIED RADIATION AND ISOTOPES, vol. 68, no. 6, 1 June 2010 (2010-06-01), pages 1060 - 1065, XP026947034, ISSN: 0969-8043, DOI: 10.1016/j.apradiso.2009.12.043
WILSON, T. C. ET AL.: "Radiosynthesis of SPECT tracers via a 1-12 copper mediated123I iodination of (hetero) ary l boron reagents", CHEMICAL COMMUNICATIONS, vol. 52, no. 90, 1 January 2016 (2016-01-01), pages 13277 - 13280, XP055628019, ISSN: 1359-7345, DOI: 10.1039/C6CC07417K
KABALKA, G. W. ET AL: "No-carrier-added radiohalogenations utilizing organoboranes: The synthesis of iodine-123 labeled curcumin", JOURNAL OF ORGANOMETALLIC CHEMISTRY, vol. 694, no. 11, 1 May 2009 (2009-05-01), pages 1638 - 1641, XP026063026, ISSN: 0022-328x, DOI: 10.1016/j.jorganchem.2008.11.040
ZHANG, P. ET AL.: "A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids", CHEMISTRY-A EUROPEAN JOURNAL, vol. 22, no. 47, 14 November 2016 (2016-11-14), pages 16783 - 16786, XP055627922, ISSN: 0947-6539, DOI: 10.1002/chem.201604105
AKULA, M. R. ET AL.: "No-carrier-added radioiodination of triolborates, water-soluble complexes of boronic acids", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 54, no. 3, 1 January 2010 (2010-01-01), pages 132 - 134, XP055673878, ISSN: 0362-4803, DOI: 10.1002/jlcr.1831
"Frontiers in Neutron Capture Therapy", 2001, SPRINGER, Boston, MA, USA, ISBN: 978-1-4613-5478-9, article VAHATALO, J. ET AL.,: "Radioiodination techniques for aromatic amino acids", pages: 835 - 838, XP009519250
NUKLEARMEDIZIN, vol. 52, 2013, pages 212 - 21
APPLIED RADIATION AND ISOTOPES, vol. 68, 2010, pages 1060 - 1065
CHEM. COMMUN., vol. 52, 2016, pages 13277 - 13280
Attorney, Agent or Firm:
TAKASHIMA, Hajime et al. (JP)
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