DK2880005T3 - Radiofluoreringsfremgangsmåde - Google Patents

Radiofluoreringsfremgangsmåde Download PDF

Info

Publication number
DK2880005T3
DK2880005T3 DK13744519.3T DK13744519T DK2880005T3 DK 2880005 T3 DK2880005 T3 DK 2880005T3 DK 13744519 T DK13744519 T DK 13744519T DK 2880005 T3 DK2880005 T3 DK 2880005T3
Authority
DK
Denmark
Prior art keywords
column
supported
polymer
tert
radiofluorination
Prior art date
Application number
DK13744519.3T
Other languages
English (en)
Inventor
Fedor Zhuravlev
Bente Mathiessen
Original Assignee
Univ Denmark Tech Dtu
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Univ Denmark Tech Dtu filed Critical Univ Denmark Tech Dtu
Application granted granted Critical
Publication of DK2880005T3 publication Critical patent/DK2880005T3/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/004—Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
    • A61K51/065—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules conjugates with carriers being macromolecules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
    • A61K51/1241—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules particles, powders, lyophilizates, adsorbates, e.g. polymers or resins for adsorption or ion-exchange resins
    • A61K51/1244—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules particles, powders, lyophilizates, adsorbates, e.g. polymers or resins for adsorption or ion-exchange resins microparticles or nanoparticles, e.g. polymeric nanoparticles
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/24—Stationary reactors without moving elements inside
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D15/00—Separating processes involving the treatment of liquids with solid sorbents; Apparatus therefor
    • B01D15/08—Selective adsorption, e.g. chromatography
    • B01D15/26—Selective adsorption, e.g. chromatography characterised by the separation mechanism
    • B01D15/36—Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/24—Stationary reactors without moving elements inside
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/11—Compounds covalently bound to a solid support

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physics & Mathematics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Nanotechnology (AREA)
  • Dispersion Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)

Claims (15)

1. Fremgangsmåde til udførelse af radiofluorering af et substrat, hvilken fremgangsmåde omfatter følgende trin: (a) etablering af kontakt mellem en vandig opløsning af [^^F] fluorid og en polymerunderstøttet phosphazenbase, der er udvalgt fra et phosphazen med den almene formel
der er understøttet på polystyren (Pps-P2^), og et phosphazen med formlen
, der er understøttet på PEG-coatet polystyren (Pps-peg-P2®^), i tilstrækkelig tid til at optage [^^F] fluorid på den polymerunderstøttede phosphazenbase; og (b) etablering af kontakt mellem en opløsning af substratet med den polymerunderstøttede phosphazenbase med [^^F] fluorid optaget derpå, der er opnået i trin (a), i tilstrækkelig tid til, at en radiofluoreringsreaktion kan finde sted.
2. Fremgangsmåde ifølge krav 1, hvor substratet, der er anvendt i trin (b), er en alifatisk eller aromatisk forbindelse omfattende en fraspaltelig gruppe.
3. Fremgangsmåde ifølge krav 2, hvor den fraspaltelige gruppe er udvalgt fra gruppen bestående af triflat, nosylat, mesylat, tosylat, chlorid, bromid, iodid og nitro.
4. Fremgangsmåde ifølge krav 2 eller krav 3, hvor forbindelsen, der omfatter den fraspaltelige gruppe, er udvalgt fra naphthylethylforbindelser, mannose, eventuelt substituerede pyridinforbindelser og glycoler.
5. Fremgangsmåde ifølge et hvilket som helst af de foregående krav, hvor den polymerunderstøttede phosphazenbase er indeholdt i en søjle.
6. Fremgangsmåde ifølge et hvilket som helst af de foregående krav, hvor den polymerunderstøttede phosphazenbase har den almene formel
der er understøttet på polystyren (Pps-Pi*^), og R er udvalgt fra gruppen bestående af methyl, ethyl, propyl, butyl, isopropyl, isobutyl, tert-butyl, pentyl, isopentyl, tert-pentyl, og tert-octyl.
7. Fremgangsmåde ifølge krav 6, hvor R er udvalgt ffa gruppen bestående af ethyl, tert-butyl og tert-octyl.
8. Fremgangsmåde ifølge et hvilket som helst af de foregående krav, hvor den polymerunderstøttede phosphazenbase er udvalgt fra Pps-P2®“
9. Fremgangsmåde ifølge et hvilket som helst af de foregående krav, hvor trin (b) omfatter opvarmning af den polymerunderstøttede phosphazenbase med [^^F] fluorid, der er optaget derpå, i kontakt med substratopløsningen til en temperatur på ifa 50 °C til 120 °C.
10. Fremgangsmåde til fremstilling af en radiotracer til administration til en patient, hvilken fremgangsmåde omfatter radiofluoreringsff emgangsmåden ifølge et hvilket som helst af kravene 1-9, efterfulgt af et trin med formulering af produktet fra trin (b) til administration til patienten.
11. Anordning til udførelse af radiofluoreringsreaktioner omfattende en polymerunderstøttet phosphazenbase, der er udvalgt fra et phosphazen med den almene formel
R=alkyl, gj. understøttet på polystyren (Pps-P2^), og et phosphazen med formlen
der er understøttet på PEG-coatet polystyren (Pps-peg-Pi^ indeholdt i en søjle.
12. Anordning ifølge krav 11, hvor R er udvalgt fra gruppen bestående af methyl, ethyl, propyl, butyl, isopropyl, isobutyl, tert-butyl, pentyl, isopentyl, tert-pentyl, og tert-octyl, og er fortrinsvis udvalgt fra gruppen bestående af ethyl, tert-butyl og tert-octyl.
13. Anordning ifølge krav 11, hvor den polymerunderstøttede phosphazenbase er udvalgt fra Pps-P2®“
14. Anvendelse af en anordning ifølge et hvilket som helst af kravene 11 til 13 ved udførelse af radiofluoreringsreaktioner.
15. Anordning til fremstilling af en dosis af en radiotracer til administration til en patient, hvilken anordning omfatter: (a) en cyclotron; (b) et radiosyntesemodul, omfattende en anordning ifølge et hvilket som helst af kravene 11 til 13; og (c) et formuleringsmodul.
DK13744519.3T 2012-07-30 2013-07-30 Radiofluoreringsfremgangsmåde DK2880005T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201200482 2012-07-30
DKPA201300319 2013-05-24
PCT/EP2013/066025 WO2014020035A1 (en) 2012-07-30 2013-07-30 Radiofluorination method

Publications (1)

Publication Number Publication Date
DK2880005T3 true DK2880005T3 (da) 2016-07-18

Family

ID=48914272

Family Applications (1)

Application Number Title Priority Date Filing Date
DK13744519.3T DK2880005T3 (da) 2012-07-30 2013-07-30 Radiofluoreringsfremgangsmåde

Country Status (4)

Country Link
US (1) US9856182B2 (da)
EP (1) EP2880005B1 (da)
DK (1) DK2880005T3 (da)
WO (1) WO2014020035A1 (da)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201518918D0 (en) 2015-10-26 2015-12-09 Norsk Medisinsk Syklotronsenter As And Uni I Oslo Method
JP2019085363A (ja) * 2017-11-06 2019-06-06 セントラル硝子株式会社 ２−デオキシ−２−フルオロ−グルコースの製造方法
GB202108605D0 (en) * 2021-06-16 2021-07-28 Ge Healthcare Uk Ltd Effect of water content

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH11295494A (ja) 1998-04-08 1999-10-29 Nippon Meji Physics Kk ［ｆ−１８］−フッ化物イオンの製造方法
GB0229686D0 (en) 2002-12-20 2003-01-29 Amersham Plc Solid-phase fluorination of benzothiazoles
GB0524851D0 (en) * 2005-12-06 2006-01-11 Ge Healthcare Ltd Radiolabelling method using polymers
KR20080072233A (ko) 2007-02-01 2008-08-06 세메스 주식회사 로봇암의 웨이퍼 감지장치
EP2017359A3 (en) 2007-06-11 2009-08-05 Trasis S.A. Method for the elution of 18F fluoride trapped on an anion-exchange resin in a form suitable for efficient radiolabeling without any evaporation step
KR101009712B1 (ko) 2007-02-22 2011-01-19 재단법인 아산사회복지재단 양성자성 용매와 이에 녹는 염들을 이용한 음이온 교환고분자 지지체로부터의 플루오린-18 플루오라이드 용리와이를 이용한 플루오린-18의 표지방법
EP1990310A1 (en) 2007-04-23 2008-11-12 Trasis S.A. Method for the preparation of reactive 18F fluoride, and for the labeling of radiotracers, using a modified non-ionic solid support and without any evaporation step
EP2062630A1 (en) 2007-11-20 2009-05-27 Trasis S.A. Method for the direct elution of reactive 18F fluoride from an anion exchange resin in an organic medium by the use of strong organic bases
FR2957345B1 (fr) 2010-03-09 2012-04-20 Polyintell Procede de preparation d'un radiotraceur

Also Published As

Publication number Publication date
WO2014020035A1 (en) 2014-02-06
US20150299066A1 (en) 2015-10-22
EP2880005B1 (en) 2016-05-25
US9856182B2 (en) 2018-01-02
EP2880005A1 (en) 2015-06-10

Similar Documents

Publication Publication Date Title
US10584078B2 (en) Dual run cassette for the synthesis of 18F-labelled compounds
JP6145107B2 (ja) 加水分解性脱保護工程及び固相抽出を含む１８ｆ−標識化合物の生産
KR102109225B1 (ko) 18f-플루시클로빈의 제조
Kim et al. Rapid synthesis of [18F] FDG without an evaporation step using an ionic liquid
US10703771B2 (en) Fluoride trapping arrangement
DK2880005T3 (da) Radiofluoreringsfremgangsmåde
US9988336B2 (en) Gaseous F-18 technologies
Kim et al. On-demand radiosynthesis of N-succinimidyl-4-[18 F] fluorobenzoate ([18 F] SFB) on an electrowetting-on-dielectric microfluidic chip for 18 F-labeling of protein
US10662125B2 (en) PET tracer purification system
Gomzina et al. Optimization of Automated synthesis of 2-[18F] Fluoro-2-deoxy-D-glucose involving base hydrolysis
US20200047158A1 (en) Solid phase conditioning
EP3538161B1 (en) Methods for multi-dose synthesis of [f-18]fddnp for clinical settings
EP3068747B1 (en) Dual run cassette for the synthesis of 18f-labelled compounds
CN117049949A (zh) 一种5-[18f](2-氟烷氧基)环辛-1-烯的合成方法
WO2023229997A1 (en) Cgmp-compliant automated [18f]fspg production for clinical examination