FLUORINATION PROCESS OF ANILIDE DERIVATIVES AND BENZOTHIAZOLE FLUORINATE DERIVATIVES AS IN VIVO IMAGING AGENTS

The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10a...

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Main Authors WILLIAMS, LORENZO, JONES, CLARE, LOUISE, BOUVET, DENIS, RAYMOND, CHRISTOPHE, KARIMI, FARHAD, LASBISTES, NICOLAS, NAIRNE, ROBERT, JAMES, STOREY, ANTHONY, EAMON, GIBSON, ALEXANDER, MARK, LANGSTROM, BENGT, FAIRWAY, STEVEN, MICHAEL
Format Patent
LanguageEnglish
French
German
Published 10.12.2014
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEAR ENGINEERING
NUCLEAR PHYSICS
NUCLEAR REACTORS
ORGANIC CHEMISTRY
PHYSICS
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, -(CH2CH2O)q-CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.
Bibliography:Application Number: EP20060765263