WO2002090298A3 - Method for the synthesis of 18f marked compounds which are low in carriers - Google Patents

Method for the synthesis of 18f marked compounds which are low in carriers Download PDF

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Publication number
WO2002090298A3
WO2002090298A3 PCT/DE2002/001548 DE0201548W WO02090298A3 WO 2002090298 A3 WO2002090298 A3 WO 2002090298A3 DE 0201548 W DE0201548 W DE 0201548W WO 02090298 A3 WO02090298 A3 WO 02090298A3
Authority
WO
WIPO (PCT)
Prior art keywords
carriers
marked
compounds
low
inventive method
Prior art date
Application number
PCT/DE2002/001548
Other languages
German (de)
French (fr)
Other versions
WO2002090298A2 (en
Inventor
Kurt Hamacher
Marianne Jelinski
Heinz H Coenen
Original Assignee
Forschungszentrum Juelich Gmbh
Kurt Hamacher
Marianne Jelinski
Heinz H Coenen
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 Forschungszentrum Juelich Gmbh, Kurt Hamacher, Marianne Jelinski, Heinz H Coenen filed Critical Forschungszentrum Juelich Gmbh
Publication of WO2002090298A2 publication Critical patent/WO2002090298A2/en
Publication of WO2002090298A3 publication Critical patent/WO2002090298A3/en

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

The invention relates to a method for the synthesis of 18F marked compounds which are low in carriers. Nucleophilic phase-transfer catalyzed 18F- fluoridation was previously the only way to produce 18F marked radiotracers having a high molar activity (> 3,7 . 1016 Bq/mol) for nuclear medicinal diagnosis. However, this marking method pre-supposes that educts having high nucleofugic leaving groups are accessible and that the requisite chemical stability of said compounds is guaranteed in said marking conditions. Complex natural substances and the derivatives thereof do not fulfil said conditions. They are irreversibly damaged or denatured. The inventive method makes it possible to mark natural substances and the derivatives thereof with 18F, especially in a stereoselective manner in mild reaction conditions. According to the inventive method, 18F marked compounds which are low in carriers can be synthesized, by 18F fluoridating perfluoroalkyl sulfonimides and by subsequent esterization with a hydroxy function. According to the inventive method it is also possible to work with small amounts of educts and therefore to increase the cost-effectiveness of the method.
PCT/DE2002/001548 2001-05-04 2002-04-26 Method for the synthesis of 18f marked compounds which are low in carriers WO2002090298A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2001121741 DE10121741A1 (en) 2001-05-04 2001-05-04 Process for the synthesis of low-carrier · 18 · F labeled compounds
DE10121741.2 2001-05-04

Publications (2)

Publication Number Publication Date
WO2002090298A2 WO2002090298A2 (en) 2002-11-14
WO2002090298A3 true WO2002090298A3 (en) 2003-03-06

Family

ID=7683635

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE2002/001548 WO2002090298A2 (en) 2001-05-04 2002-04-26 Method for the synthesis of 18f marked compounds which are low in carriers

Country Status (2)

Country Link
DE (1) DE10121741A1 (en)
WO (1) WO2002090298A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011526267A (en) * 2008-07-03 2011-10-06 バイエル ファーマ アクチエンゲゼルシャフト Compound and radiopharmaceutical production method
GB0812923D0 (en) * 2008-07-15 2008-08-20 Isis Innovation Preparation of flourine-labelled compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994024098A1 (en) * 1993-04-20 1994-10-27 Schering Aktiengesellschaft Ξ-fluorosulphonimides, method of preparing them and their use as fluorination agents
WO1999011590A1 (en) * 1997-09-03 1999-03-11 Immunomedics, Inc. Fluorination of proteins and peptides for f-18 positron emission tomography

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3424525A1 (en) * 1984-07-04 1986-01-16 Kernforschungsanlage Jülich GmbH, 5170 Jülich METHOD FOR PRODUCING (ARROW UP) 1 (ARROW UP) (ARROW UP) 8 (ARROW UP) F-ALKYL AND ARYL COMPOUNDS BY HALOGEN EXCHANGE
US6248889B1 (en) * 1998-11-20 2001-06-19 3M Innovative Properties Company Process for converting an alcohol to the corresponding fluoride

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994024098A1 (en) * 1993-04-20 1994-10-27 Schering Aktiengesellschaft Ξ-fluorosulphonimides, method of preparing them and their use as fluorination agents
WO1999011590A1 (en) * 1997-09-03 1999-03-11 Immunomedics, Inc. Fluorination of proteins and peptides for f-18 positron emission tomography

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BENNUA-SKALMOWSKI B ET AL: "A facile conversion of primary or secondary alcohols with n-perfluorobutanesulfonyl fluoride/1,8-diazabicyclo[5.4.0]undec-7-ene into their corresponding fluorides", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 36, no. 15, 1995, pages 2611 - 2613, XP002120040, ISSN: 0040-4039 *

Also Published As

Publication number Publication date
WO2002090298A2 (en) 2002-11-14
DE10121741A1 (en) 2002-11-14

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