Title:
METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO, AND PRECURSOR OF 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO
Document Type and Number:
WIPO Patent Application WO/2015/129374
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide: a novel method for producing 18F-labeled 4-boronophenylalanine (BPA); and a precursor of 18F-labeled BPA. 18F-labeled BPA can be prepared by preparing a compound represented by formula (1) and using the compound. In the formula, R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3
- or BX3
-M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).
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Inventors:
TAKENAKA HIROSHI (JP)
OHTA YOICHIRO (JP)
TAGUCHI YUSUKE (JP)
UEDA SAYURI (JP)
ISHINO YUKO (JP)
YOSHIKAWA TOMOHIRO (JP)
NAKASHIMA HIDEKI (JP)
UEHARA KOHKI (JP)
KIRIHATA MITSUNORI (JP)
OHTA YOICHIRO (JP)
TAGUCHI YUSUKE (JP)
UEDA SAYURI (JP)
ISHINO YUKO (JP)
YOSHIKAWA TOMOHIRO (JP)
NAKASHIMA HIDEKI (JP)
UEHARA KOHKI (JP)
KIRIHATA MITSUNORI (JP)
Application Number:
PCT/JP2015/052303
Publication Date:
September 03, 2015
Filing Date:
January 28, 2015
Export Citation:
Assignee:
STELLA PHARMA CORP (JP)
UNIV OSAKA PREFECT PUBLIC CORP (JP)
UNIV OSAKA PREFECT PUBLIC CORP (JP)
International Classes:
C07C47/55; C07B59/00; C07C45/63; C07F5/02
Domestic Patent References:
| WO2014061508A1 | 2014-04-24 |
Foreign References:
| CN102887913A | 2013-01-23 |
Other References:
JYRKI K. VAHATALO ET AL.: "Synthesis of 4- dihydroxyboryl-2-[18F] fluorophenylalanine with relatively high-specific activity", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 45, 2002, pages 697 - 704, XP055221872
KIICHI ISHIKAWA ET AL.: "Synthesis and Radiation Dosimetry of 4-Brono-2-[18F]fluoro-D,L- phenylalanine: a Target Compound for PET and Boron Neutron Capture Therapy", APPLIED RADIATION AND ISOTOPES, vol. 42, no. 4, 1991, pages 325 - 328, XP024725815
M. J. AL-DARWICH ET AL.: "Enantioselective syntheses of no-carrier-added (n.c.a.) (S)-4- chloro-2-[18F]fluorophenylalanine and (S)-(a- methy)-4-chloro-2-[18F]fluorophenylalanine", JOURNAL OF FLUORINE CHEMISTRY, vol. 80, 1996, pages 117 - 124, XP004071319
HIROSHI FUKUDA: "Development of positron emitter labeled agents for boron neutron capture therapy", KAGAKU KENKYUHI JOSEI JIGYO (GAKUJUTSU KENKYU JOSEI KIKIN JOSEIKIN) KENKYU SEIKA HOKOKUSHO, 3 March 2015 (2015-03-03), XP008184642, Retrieved from the Internet
KIICHI ISHIKAWA ET AL.: "Synthesis and Radiation Dosimetry of 4-Brono-2-[18F]fluoro-D,L- phenylalanine: a Target Compound for PET and Boron Neutron Capture Therapy", APPLIED RADIATION AND ISOTOPES, vol. 42, no. 4, 1991, pages 325 - 328, XP024725815
M. J. AL-DARWICH ET AL.: "Enantioselective syntheses of no-carrier-added (n.c.a.) (S)-4- chloro-2-[18F]fluorophenylalanine and (S)-(a- methy)-4-chloro-2-[18F]fluorophenylalanine", JOURNAL OF FLUORINE CHEMISTRY, vol. 80, 1996, pages 117 - 124, XP004071319
HIROSHI FUKUDA: "Development of positron emitter labeled agents for boron neutron capture therapy", KAGAKU KENKYUHI JOSEI JIGYO (GAKUJUTSU KENKYU JOSEI KIKIN JOSEIKIN) KENKYU SEIKA HOKOKUSHO, 3 March 2015 (2015-03-03), XP008184642, Retrieved from the Internet
Attorney, Agent or Firm:
UNIUS PATENT ATTORNEYS OFFICE (JP)
Patent business corporation ユニアス international patent firm (JP)
Patent business corporation ユニアス international patent firm (JP)
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