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US 2013/0172620 A1Published application
Method for production of f-18 labeled amyloid beta ligands
AssigneePiramal Imaging SA
InventorsMathias Berndt, Matthias Friebe, Christina Hultsch, Fabrice Samson, Marianne Patt, Andreas Schildan, Christoph Smuda
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Abstract
This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.
Claims15
A Method for producing a compound of Formula I
- comprising the steps of:
- Step 1:
- Radiolabeling compound of Formula II with a F-18 fluorinating agent, to obtain compound of Formula I, if R═H or to obtain compound of Formula III, if R=PG
- Step 2:
- If R=PG, cleavage of the protecting group PG to obtain a compound of Formula I,
- Step 3:
- Purification and Formulation of a compound of Formula I,
- wherein:
- n=1-6,
- X is selected from the group consisting of
- a) CH,
- b) N,
- R is selected from the group consisting of
- a) H,
- b) PG,
- PG is an “Amine-protecting group”,
- LG is a leaving group,
- wherein LG contains 0-3 fluorine atoms,
- wherein the radiofluorination reaction is carried out in acetonitrile, or in a mixture of acetonitrile and a co-solvent.
16 more elements
Dependencies are inferred from the claim text.