Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes

The present invention provides novel alpha-fluoroalkyl compounds having structure I and the corresponding dihydrotetrabenazine compounds IV and intermediates useful in the preparation of such compounds. The alpha-fluoroalkyl compounds are provided in both racemic and enantiomerically enriched forms...

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Bibliographic Details
Main Authors JOHNSON BRUCE FLETCHER, RISHEL MICHAEL JAMES, AMARASINGHE KANDE KANKANANAMAL, DINN SEAN RICHARD
Format Patent
LanguageChinese
English
Published 29.05.2013
Subjects
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The present invention provides novel alpha-fluoroalkyl compounds having structure I and the corresponding dihydrotetrabenazine compounds IV and intermediates useful in the preparation of such compounds. The alpha-fluoroalkyl compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The alpha-fluoroalkyl compounds are shown to possess high affinity for VMAT-2, a biomarker implicated, for example, in human diabetes. The alpha-fluoroalkyl compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled alpha-fluoroalkyl compounds are useful as probes for the discovery of PET imaging agents.
Bibliography:Application Number: CN200880118894