CN1938244B - 氟化方法 - Google Patents

氟化方法 Download PDF

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Publication number
CN1938244B
CN1938244B CN200580010361.3A CN200580010361A CN1938244B CN 1938244 B CN1938244 B CN 1938244B CN 200580010361 A CN200580010361 A CN 200580010361A CN 1938244 B CN1938244 B CN 1938244B
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China
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alkyl
water
fluoride
heteroaryl
acetonitrile
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Expired - Fee Related
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CN200580010361.3A
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Chinese (zh)
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CN1938244A (zh
Inventor
H·J·瓦德斯沃思
T·德弗尼什
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GE Healthcare Ltd
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GE Healthcare Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C277/08—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
    • 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
    • C07B59/001—Acyclic or carbocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C17/00—Preparation of halogenated hydrocarbons
    • C07C17/361—Preparation of halogenated hydrocarbons by reactions involving a decrease in the number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
    • C07C51/363—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20—Spiro-condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
CN200580010361.3A 2004-04-08 2005-04-06 氟化方法 Expired - Fee Related CN1938244B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0407952.1 2004-04-08
GBGB0407952.1A GB0407952D0 (en) 2004-04-08 2004-04-08 Fluoridation method
PCT/GB2005/001344 WO2005097713A1 (en) 2004-04-08 2005-04-06 Fluoridation method

Publications (2)

Publication Number Publication Date
CN1938244A CN1938244A (zh) 2007-03-28
CN1938244B true CN1938244B (zh) 2013-03-13

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CN200580010361.3A Expired - Fee Related CN1938244B (zh) 2004-04-08 2005-04-06 氟化方法

Country Status (6)

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US (2) US7935852B2 (https=)
EP (1) EP1732865A1 (https=)
JP (1) JP2007532524A (https=)
CN (1) CN1938244B (https=)
GB (1) GB0407952D0 (https=)
WO (1) WO2005097713A1 (https=)

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GB0329716D0 (en) * 2003-12-23 2004-01-28 Amersham Plc Radical trap
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GB0524851D0 (en) * 2005-12-06 2006-01-11 Ge Healthcare Ltd Radiolabelling method using polymers
PT2146944E (pt) * 2007-04-11 2014-03-11 Merck & Cie Processo para a preparação de folatos marcados com 18f
KR20100022987A (ko) * 2007-06-20 2010-03-03 지이 헬쓰케어 리미티드 표지 방법
MX2010005122A (es) * 2007-11-07 2010-08-18 Ge Healthcare Bv Estabilizacion de radiofarmaceuticos.
US8980221B2 (en) 2008-01-03 2015-03-17 Ge Healthcare Limited Fluoride processing method
GB0808986D0 (en) 2008-05-16 2008-06-25 Univ Newcastle Formation of 18F and 19F fluoroarenes bearing reactive functionalities
EP2303897A4 (en) * 2008-06-05 2012-02-22 Harvard College HIGH VALENCIA PALLADIUM FLUORIDE COMPLEXES AND USES THEREOF
WO2010008522A2 (en) 2008-07-14 2010-01-21 The Regents Of The University Of California Nucleophilic fluorination of aromatic compounds
WO2010015340A1 (en) * 2008-08-06 2010-02-11 Bayer Schering Pharma Aktiengesellschaft Daa-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
GB0814893D0 (en) * 2008-08-14 2008-09-17 Ge Healthcare Ltd Improved fluoridation of iodonium salts
CN101723849B (zh) * 2008-10-10 2012-11-21 北京师范大学 18f标记氨基酸类衍生物、其制备方法及其制备报告肿瘤的正电子发射断层显像分子探针中的应用
CN101723850B (zh) * 2008-10-10 2012-11-21 北京师范大学 18f标记芳香氨基酸及其制备方法和肿瘤显像应用
JP4358892B1 (ja) * 2008-10-16 2009-11-04 エア・ウォーター株式会社 フッ化処理方法およびフッ化処理装置ならびにフッ化処理装置の使用方法
GB0819293D0 (en) * 2008-10-21 2008-11-26 Hammersmith Imanet Ltd Radiofluorination
US9302990B2 (en) * 2008-10-21 2016-04-05 Nutech Ventures Fluorination of aromatic ring systems
EP3284736B1 (en) 2008-10-21 2021-03-03 NUtech Ventures Fluorination of aromatic ring systems
WO2010059943A2 (en) 2008-11-20 2010-05-27 President And Fellows Of Harvard College Fluorination of organic compounds
AU2010203461A1 (en) * 2009-01-09 2011-07-28 President And Fellows Of Harvard College Fluorine containing compounds and methods of use thereof
GB0917611D0 (en) * 2009-10-08 2009-11-25 Ge Healthcare Ltd Automated radiosynthesis
US8377704B2 (en) 2009-10-20 2013-02-19 Nutech Ventures Detection and quantification of anions
IN2012DN04871A (https=) 2009-12-11 2015-09-25 Semiconductor Energy Laoboratory Co Ltd
US8546578B2 (en) * 2010-02-04 2013-10-01 Nutech Ventures Iodonium Cyclophanes for SECURE arene functionalization
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US9273083B2 (en) 2012-09-26 2016-03-01 President And Fellows Of Harvard College Nickel fluorinating complexes and uses thereof
US9266847B2 (en) * 2012-11-09 2016-02-23 Vanderbilt University Compounds, probes, and methods of synthesis and methods of imaging COX-2-associated diseases
ITTO20120996A1 (it) * 2012-11-16 2014-05-17 Consiglio Nazionale Ricerche Procedimento e impianto per la produzione di radiotraccianti pet 18f-fluorurati
WO2015058047A2 (en) 2013-10-18 2015-04-23 President And Fellows Of Harvard College Fluorination of organic compounds
CN106536490A (zh) * 2014-01-03 2017-03-22 纽泰克温图斯公司 放射性碘代化合物
US20150367005A1 (en) * 2014-06-19 2015-12-24 The Regents Of The University Of Michigan Method of synthesizing fluorine-18 labeled radiopharmaceuticals in ethanol and water
AU2016360886B2 (en) * 2015-11-24 2021-04-15 Centre National De La Recherche Scientifique Method for synthesizing iodo- or astatoarenes using diaryliodonium salts
US11628229B2 (en) * 2017-03-13 2023-04-18 Arizona Board Of Regents On Behalf Of The University Of Arizona Method of synthesizing 18F radiolabeled biomolecular agents
KR102031652B1 (ko) * 2018-01-19 2019-10-14 서울대학교산학협력단 전이체 단백질 과발현 관련 질환의 양성자방출단층촬영 방사성추적자, 형광영상 진단 및 광역학 치료를 위한 전이체 단백질 표적 리간드 및 이의 제조방법
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Publication number Publication date
GB0407952D0 (en) 2004-05-12
EP1732865A1 (en) 2006-12-20
CN1938244A (zh) 2007-03-28
US20110196149A1 (en) 2011-08-11
JP2007532524A (ja) 2007-11-15
US20070092441A1 (en) 2007-04-26
WO2005097713A1 (en) 2005-10-20
US7935852B2 (en) 2011-05-03

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